VEGFR Inhibitors (inhibitors, agonists and modulators)...Tel: 1-631-504-6093 Fax: 1-631-614-7828 E-mail: [email protected] 45-16 Ramsey Road Shirley, NY 11967, USA VEGFR Inhibitors (inhibitors,

Tel: 1-631-504-6093 Fax: 1-631-614-7828

E-mail: [email protected]

45-16 Ramsey Road Shirley, NY 11967, USA

VEGFR Inhibitors

(inhibitors, agonists and modulators)

Vascular endothelial growth factor (VEGF) is an important signaling protein involved in both vasculogenesis (the formation

of the circulatory system) and angiogenesis (the growth of blood vessels from pre-existing vasculature).

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Sorafenib - CAS 284461-73-0

Catalog Number: B0084-065081 Price: $149/1 g

Molecular Weight: 464.82 Molecular Formula: C21H16ClF3N4O3

Description: Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.

BIBF 1202 - CAS 894783-71-2

Catalog Number: B0084-474893 Price: $458/50 mg

Molecular Weight: 525.60 Molecular Formula: C30H31N5O4

Description: BIBF 1202 is the major in-vivo metabolite of BIBF 1120, which is an oral triple angiokinase inhibitor targeting VEGFR, PDGFR, FGFR. It is a related compound of Intedanib, which

is an indolinone derivative that inhibits angiokinase and an antitumor agent. It is a novel

treatment modality in oncology through blockade of the vascular endothelial growth factor

(VEGF) signaling pathway thus inhibition of tumor angiogenesis.

SU 4312 - CAS 5812-07-7


Molecular Weight: 264.33 Molecular Formula: C17H16N2O

Description: SU 4312 is a potent and selective inhibitor of VEGFR and PDGFR tyrosine kinases (IC50 = 0.8 and 19.4 μM, respectively) wirth selectivity over EGFR and c-Src tyrosine kinases.

Semaxanib - CAS 204005-46-9



Description: Semaxanib is a quinolone derivative with potential antineoplastic activity. Semaxanib reversibly inhibits ATP binding to the tyrosine kinase domain of vascular endothelial

growth factor receptor 2 (VEGFR2), which may inhibit VEGF-stimulated endothelial cell migration

and proliferation and reduce the tumor microvasculature. This agent also inhibits the

phosphorylation of the stem cell factor receptor tyrosine kinase c-kit, often expressed in acute

myelogenous leukemia cells.

https://www.bocsci.com/sorafenib-cas-284461-73-0-item-65081.htmlhttps://www.bocsci.com/bibf-1202-cas-894783-71-2-item-474893.htmlhttps://www.bocsci.com/su-4312-cas-5812-07-7-item-357203.htmlhttps://www.bocsci.com/semaxanib-cas-204005-46-9-item-352931.html

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OSI-930 - CAS 728033-96-3


Molecular Weight: 443.444 Molecular Formula: C22H16F3N3O2S

Description: OSI-930 is a selective thiophene-derived tyrosine kinase inhibitor with potential antineoplastic activity. Tyrosine kinase inhibitor OSI-930 inhibits stem cell factor receptor (c-Kit)

and the vascular endothelial growth factor receptor 2 (VEGFR2), which may result in the inhibition

of both tumor cell proliferation and tumor angiogenesis. Both c-Kit and VEGFR2 are

overexpressed in a variety of cancers.

WHI-P180 - CAS 211555-08-7



Description: WHI-P180 moderately inhibited ABCG2 function, exhibiting weak phototoxicity. The elimination half-life of WHI-P180 in CD-1 mice (BALB/ c mice) following i.v., i.p., or p.o.

administration was less than 10 min. Systemic clearance of WHI-P180 was 6742 mL/h/kg in CD-I

mice and 8188 mL/h/kg in BALB/c mice. Notably, WHI-P180, when administered in two consecutive

nontoxic i.p. bolus doses of 25 mg/kg, inhibited IgE/antigen-induced vascular hyperpermeability

in a well-characterized murine model of passive cutaneous anaphylaxis.

BIBF 1120 esylate - CAS 656247-18-6


Molecular Weight: 649.76 Molecular Formula: C33H39N5O7S

Description: Nintedanib esylate is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β.

Motesanib - CAS 453562-69-1



Description: Motesanib is a multikinase inhibitor that selectively targets VEGF receptors, platelet-derived growth factor receptors (PDGFRs), and Kit receptors. It also potently inhibits angiogenesis

and induces regression in tumor xenografts.

https://www.bocsci.com/osi-930-cas-728033-96-3-item-286626.htmlhttps://www.bocsci.com/whi-p180-cas-211555-08-7-item-312568.htmlhttps://www.bocsci.com/bibf-1120-esylate-cas-656247-18-6-item-434827.htmlhttps://www.bocsci.com/motesanib-cas-453562-69-1-item-69090.html

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hVEGF-IN-1 - CAS 1637443-98-1



Description: hVEGF-IN-1 inhibits human VEGF-A translation and has antitumor activity. Tumor bearing mice treated with hVEGF-IN-1 have an average tumor volume of less than 300 mm. The

tumor weight in the presence of hVEGF-IN-1 reduces around 60.1% to a final weight of 0.18 g. No

significant change in body weight is observed during the treatment.

Ponatinib - CAS 943319-70-8


Molecular Weight: 532.56 Molecular Formula: C29H27F3N6O

Description: Ponatinib is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM, respectively.

SU 4942 - CAS 76086-99-2


Molecular Weight: 300.155 Molecular Formula: C15H10BrNO

Description: SU 4942 is a modulator of tyrosine kinase signal transduction, targeting VEGF and ECGF.

Motesanib Diphosphate - CAS 857876-30-3


Molecular Weight: 569.44 Molecular Formula: C22H29N5O9P2

Description: Motesanib Diphosphate is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit, ~10-fold more selective for VEGFR

than PDGFR and Ret.

AG 1406 - CAS 71308-34-4



Description: AG 1406 is an inhibitor of tyrosine phosphorylation.

https://www.bocsci.com/hvegf-in-1-cas-1637443-98-1-item-267747.htmlhttps://www.bocsci.com/ponatinib-cas-943319-70-8-item-272000.htmlhttps://www.bocsci.com/su-4942-cas-76086-99-2-item-284846.htmlhttps://www.bocsci.com/motesanib-diphosphate-cas-857876-30-3-item-153042.htmlhttps://www.bocsci.com/ag-1406-cas-71308-34-4-item-284859.html

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Sunitinib Malate - CAS 341031-54-7


Molecular Weight: 532.56 Molecular Formula: C22H27FN4O2.C4H6O5

Description: Sunitinib (marketed as Sutent by Pfizer, and previously known as SU11248) is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor that was approved by the

FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal

stromal tumor (GIST) on January 26, 2006. Sunitinib was the first cancer drug simultaneously

approved for two different indications.

Nintedanib - CAS 656247-17-5



Description: Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM.

It exhibits potential antiangiogenic and antineoplastic activities.

SU 5205 - CAS 3476-86-6


Molecular Weight: 239.249 Molecular Formula: C15H10FNO

Description: SU5205 is a VEGFR2 inhibitor.

Toceranib phosphate - CAS 874819-74-6


Molecular Weight: 494.45 Molecular Formula: C22H28FN4O6P

Description: Toceranib phosphate is a kinase inhibitor with both antitumor and antiangiogenic activity through inhibition of KIT, vascular endothelial growth factor receptor 2, and PDGFRβ. It is

a receptor tyrosine kinase inhibitor and is used in the treatment of canine mast cell tumor also

called mastocytoma. It may also have an anti-angiogenic effect.

https://www.bocsci.com/sunitinib-malate-cas-341031-54-7-item-187069.htmlhttps://www.bocsci.com/nintedanib-cas-656247-17-5-item-262244.htmlhttps://www.bocsci.com/su-5205-cas-3476-86-6-item-284844.htmlhttps://www.bocsci.com/toceranib-phosphate-cas-874819-74-6-item-463666.html

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JK-P3 - CAS 942655-44-9



Description: JK-P3 is a VEGFR2 inhibitor with IC50 values of 7.8 μM. JK-P3 inhibits FGFR 1/3 kinase activity in vitro, but exhibits no effect on FGFR signaling in cell-based assays. It suppresses wound

healing and tube formation in HUVEC without effecting endothelial cell proliferation.

KDR-in-4 - CAS 408502-06-7

Catalog Number: B0084-007571


Description: A potent kinase insert domain-containing receptor (KDR/VEGFR2) inhibitor (IC50= 7 nM)

Sulfatinib - CAS 1308672-74-3



Description: Sulfatinib, an oral drug candidate, is a small molecule inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3, and the fibroblast growth factor receptor

type 1 (FGFR1). Sulfatinib exhibited an acceptable safety profile and encouraging antitumor

activity in patients with advanced solid tumors, particularly neuroendocrine tumors.

Vatalanib succinate - CAS 212142-18-2


Molecular Weight: 464.9 Molecular Formula: C20H15ClN4.C4H6O4

Description: Vatalanib succinate is a potent and orally bioactive VEGFR inhibitor (IC50 =37 and 77 nM for VEGFR-2 and -1, respectively) exhibiting potential antineoplastic activity. Vatalanib

binds to the protein kinase domain of VEGFR, and inhibits proliferation, migration and survival of

HUVECs in vitro. Vatalanib also inhibits PDGFR-β, c-Kit and c-Fms.

https://www.bocsci.com/jk-p3-cas-942655-44-9-item-284855.htmlhttps://www.bocsci.com/kdr-in-4-cas-408502-06-7-item-7571.htmlhttps://www.bocsci.com/sulfatinib-cas-1308672-74-3-item-7822.htmlhttps://www.bocsci.com/vatalanib-succinate-cas-212142-18-2-item-14541.html

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E 3810 dihydrochloride


Molecular Weight: 516.42 Molecular Formula: C26H25N3O4.2HCl

Description: E 3810 dihydrochloride is a dual VEGFR/FGFR tyrosine kinase inhibitor. It suppresses the tumor angiogenesis and tumor cell proliferation via inhibiting VEGFR1, -2, and -3 and FGFR-1

and -2 kinases in the nanomolar range.

Cediranib dihydrochloride - CAS 288383-20-0


Molecular Weight: 450.5 Molecular Formula: C25H27FN4O3

Description: Cediranib (AZD-2171; tentative trade name Recentin) is a potent inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinases.The drug is being developed by

AstraZeneca as a possible anti-cancer chemotherapeutic agent for oral administration.

Pazopanib - CAS 444731-52-6



Description: Pazopanib is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM,

respectively.

Sorafenib Tosylate - CAS 475207-59-1


Molecular Weight: 637.03 Molecular Formula: C21H16ClF3N4O3.C7H8O3S

Description: Sorafenib Tosylate (Bay 43-9006) is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.

Chloropyramine hydrochloride - CAS 6170-42-9


Molecular Weight: 326.26 Molecular Formula: C16H20ClN3.HCl

Description: Chloropyramine hydrochloride

https://www.bocsci.com/e-3810-dihydrochloride-item-54865.htmlhttps://www.bocsci.com/cediranib-dihydrochloride-cas-288383-20-0-item-84-65171.htmlhttps://www.bocsci.com/pazopanib-cas-444731-52-6-item-68950.htmlhttps://www.bocsci.com/sorafenib-tosylate-cas-475207-59-1-item-69361.htmlhttps://www.bocsci.com/chloropyramine-hydrochloride-cas-6170-42-9-item-73277.html

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Vatalanib dihydrochloride - CAS 212141-51-0


Molecular Weight: 419.73 Molecular Formula: C20H15ClN4.2HCl

Description: Vatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4.

SU5402 - CAS 215543-92-3



Description: SU5402 is a potent and selective vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR) inhibitor.

CP-547632 - CAS 252003-65-9


Molecular Weight: 532.405 Molecular Formula: C20H24BrF2N5O3S

Description: CP-547632 is as a potent inhibitor of the VEGFR-2 and basic fibroblast growth factor (FGF) kinases (IC50 11 and 9 nM, respectively). It is selective relative to epidermal growth factor

receptor, platelet-derived growth factor, and other related TKs. It also inhibits VEGF-stimulated

autophosphorylation of VEGFR-2 in a whole cell assay with an IC50 value of 6 nM. After oral

administration of CP-547,632 to mice bearing NIH3T3/H-ras tumors, VEGFR-2 phosphorylation in

tumors was inhibited in a dose-dependent fashion (EC50 590 ng/ml). CP-547,632 is a well-

tolerated, orally-bioavailable inhibitor presently under clinical investigation for the treatment of

human malignancies.

Dovitinib - CAS 405169-16-6


Molecular Weight: 392.429 Molecular Formula: C21H21FN6O

Description: Dovitinib (TKI258) potently inhibited FLT3, c-KIT, FGFR, VEGFR1/2/3, PDGFRß and CSF-1R with IC50 values of 1, 2, 5, 10, 8, 27, 36 nM respectively. Dovitinib selectively blocked the

growth of wild-type (WT) or activated mutant FGFR3-transformed B9 cells and human myeloma

cell lines. Dovitinib was an effective treatment in a xenograft mouse model of FGFR3 multiple

myeloma.

https://www.bocsci.com/vatalanib-dihydrochloride-cas-212141-51-0-item-84-87399.htmlhttps://www.bocsci.com/su5402-cas-215543-92-3-item-84-87527.htmlhttps://www.bocsci.com/cp-547632-cas-252003-65-9-item-88558.htmlhttps://www.bocsci.com/dovitinib-cas-405169-16-6-item-91881.html

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Lenvatinib - CAS 417716-92-8


Molecular Weight: 426.85 Molecular Formula: C21H19ClN4O4

Description: Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3

against FGFR1, PDGFRα/β.

Telatinib - CAS 332012-40-5



Description: Telatinib is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively.

H-Glu-Trp-OH - CAS 38101-59-6



Description: H-Glu-Trp-OH inhibits VEGF, which may inhibit angiogenesis.

(E)-FeCP-oxindole - CAS 884338-18-5


Molecular Weight: 329.17 Molecular Formula: C19H15FeNO

Description: (E)-FeCP-oxindole is a human vascular endothelial cell growth factor receptor 2 (VEGFR-2) inhibitor (IC50 = 214 nM). (E)-FeCP-oxindole exhibits anticancer activity (IC50< 1 μM

against B16 murine melanoma lines).

(Z)-FeCP-oxindole - CAS 1137967-28-2


Molecular Weight: 329.17 Molecular Formula: C19H15FeNO

Description: (Z)-FeCP-oxindole is a human vascular endothelial cell growth factor receptor 2 (VEGFR-2) inhibitor (IC50 = 220 nM). (Z)-FeCP-oxindole exhibits anticancer activity (IC50< 1 μM

against B16 murine melanoma lines).

https://www.bocsci.com/lenvatinib-cas-417716-92-8-item-92131.htmlhttps://www.bocsci.com/telatinib-cas-332012-40-5-item-108953.htmlhttps://www.bocsci.com/h-glu-trp-oh-cas-38101-59-6-item-114382.htmlhttps://www.bocsci.com/e-fecp-oxindole-cas-884338-18-5-item-119097.htmlhttps://www.bocsci.com/z-fecp-oxindole-cas-1137967-28-2-item-119101.html

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BMS 605541 - CAS 639858-32-5


Molecular Weight: 401.43 Molecular Formula: C19H17F2N5OS

Description: BMS 605541 is a potent and ATP-competitive VEGFR-2 inhibitor (IC50 = 23 nM) displaying >10-fold selectivity for VEGFR-2 over VEGFR-1. It exhibits antitumor activity in human

lung and colon tumor xenograft models.

Pazopanib HCl - CAS 635702-64-6


Molecular Weight: 473.98 Molecular Formula: C21H23N7O2·HCl

Description: Pazopanib is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM,

respectively.

Brivanib - CAS 649735-46-6



Description: Brivanib is the hydrolyzed form of Brivanib alaninate, which is a vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with potential antineoplastic activity. Brivanib

strongly binds to and inhibits VEGFR2, a tyrosine kinase receptor expressed almost exclusively on

vascular endothelial cells; inhibition of VEGFR2 may result in inhibition of tumor angiogenesis,

inhibition of tumor cell growth, and tumor regression. Check for active clinical trials or closed

clinical trials using this agent.

Brivanib alaninate - CAS 649735-63-7



Description: Brivanib alaninate is the alaninate ester of a vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with potential antineoplastic activity. Brivanib strongly binds to and

inhibits VEGFR2, a tyrosine kinase receptor expressed almost exclusively on vascular endothelial

cells; inhibition of VEGFR2 may result in inhibition of tumor angiogenesis, inhibition of tumor cell

growth, and tumor regression. Check for active clinical trials or closed clinical trials using this

agent.

https://www.bocsci.com/bms-605541-cas-639858-32-5-item-119119.htmlhttps://www.bocsci.com/pazopanib-hcl-cas-635702-64-6-item-146188.htmlhttps://www.bocsci.com/brivanib-cas-649735-46-6-item-84-146707.htmlhttps://www.bocsci.com/brivanib-alaninate-cas-649735-63-7-item-84-146708.html

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Regorafenib - CAS 755037-03-7



Description: Regorafenib, also known as BAY 73-4506, is an orally bioavailable small molecule with potential antiangiogenic and antineoplastic activities. Regorafenib binds to and inhibits vascular

endothelial growth factor receptors (VEGFRs) 2 and 3, and Ret, Kit, PDGFR and Raf kinases, which

may result in the inhibition of tumor angiogenesis and tumor cell proliferation. VEGFRs are

receptor tyrosine kinases that play important roles in tumor angiogenesis; the receptor tyrosine

kinases RET, KIT, and PDGFR, and the serine/threonine-specific Raf kinase are involved in tumor

cell signaling. Regorafenib is demonstrated to increase the overall survival of patients with

metastatic colorectal cancer and has been approved by the US FDA on September 27, 2012.

Linifanib - CAS 796967-16-3



Description: Description of Linifanib: Linifanib is an orally bioavailable, small-molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. Linifanib inhibits members of

the vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF) receptor

families; it exhibits much less activity against unrelated RTKs, soluble tyrosine kinases, or

serine/threonine kinases. This agent does not have a general antiproliferative effect due to its

high dose requirement. However, linifanib may exhibit potent antiproliferative and apoptotic

effects on tumor cells whose proliferation is dependent on mutant kinases, such as fms-related

tyrosine kinase receptor-3 (FLT3).

foretinib - CAS 849217-64-7


Molecular Weight: 632.665 Molecular Formula: C34H34F2N4O6

Description: Potent inhibitor of MET, VEGFR2, Ron and AXL (IC50 values are 0.4, 0.9, 3 and 11 nM, respectively). Also potently inhibits Tie-2, Flt-1, Flt-3, Flt-4, KIT, PDGFRalpha and PDGFRbeta.

Inhibits migration and invasion of B16F10 melanoma cells in vitro. Suppresses B16F10 tumor growth

and metastasis in mice.

https://www.bocsci.com/regorafenib-cas-755037-03-7-item-151007.htmlhttps://www.bocsci.com/linifanib-cas-796967-16-3-item-151820.htmlhttps://www.bocsci.com/foretinib-cas-849217-64-7-item-152657.html

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MGCD-265 - CAS 875337-44-3


Molecular Weight: 517.60 Molecular Formula: C26H20FN5O2S2

Description: MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively and also inhibits Ron and Tie2.

ENMD-2076 - CAS 934353-76-1


Molecular Weight: 375.47 Molecular Formula: C21H25N7

Description: ENMD-2076 is an orally-active, Aurora A/angiogenic kinase inhibitor with a unique kinase selectivity profile and multiple mechanisms of action. ENMD-2076 has been shown to

inhibit a distinct profile of angiogenic tyrosine kinase targets in addition to the Aurora A kinase.

Aurora kinases are key regulators of mitosis (cell division), and are often over-expressed in human

cancers. ENMD-2076 also targets the VEGFR, Flt-3 and FGFR3 kinases which have been shown to

play important roles in the pathology of several cancers. ENMD-2076 has shown promising

activity in Phase 1 clinical trials in solid tumor cancers, leukemia, and multiple myeloma. ENMD-

2076 is currently in a Phase 2 trial for ovarian cancer, and preclinical and clinical activities are

ongoing in assessing the compound's applicability for other forms of cancer.

ZM 306416 hydrochloride - CAS 196603-47-1


Molecular Weight: 370.21 Molecular Formula: C16H13N3O2FCl.HCl

Description: ZM 306416 hydrochloride is an inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinase with > 3-fold selectivity over FGFR-1. ZM 306416 hydrochloride inhibits

activity of KDR and FLT VEGF receptors (IC50 = 100 nM and 2 μM, respectively).

Ki8751 - CAS 228559-41-9



Description: Ki8751 is a potent, selective inhibitor of VEGFR-2 tyrosine kinase (IC50 = 0.9 nM). Displays some inhibitory activity towards c-Kit, PDGFRα and FGFR-2 (IC50 values range from 40

to 170 nM).

https://www.bocsci.com/mgcd-265-cas-875337-44-3-item-153700.htmlhttps://www.bocsci.com/enmd-2076-cas-934353-76-1-item-156198.htmlhttps://www.bocsci.com/zm-306416-hydrochloride-cas-196603-47-1-item-170446.htmlhttps://www.bocsci.com/ki8751-cas-228559-41-9-item-84-175350.html

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NVP-ACC789 - CAS 300842-64-2


Molecular Weight: 405.3 Molecular Formula: C21H17BrN4

Description: NVP-ACC789 is a potent, selective and orally active inhibitor of the VEGF receptor tyrosine kinases, antagonizing tumor-driven angiogenesis

Ramucirumab - CAS 947687-13-0


Molecular Weight: 143609.68 Molecular Formula: C6374H9864N1692O1996S46

Description: Ramucirumab is a human IgG1 monoclonal antibody developed by ImClone Systems Inc to treat solid tumors. It has been approved by FDA for the treatment of advanced gastric or

gastro-esophageal junction adenocarcinoma and metastatic non-small-cell lung carcinoma

(NSCLC). Ramucirumab acts as a VEGFR2 antagonist via binding to VEGFR2.

Sunitinib - CAS 557795-19-4



Description: Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit.

Tanshinone IIA - CAS 568-72-9


Molecular Weight: 294.34 Molecular Formula: C19H18O3

Description: Tanshinone IIA, under the IUPAC name 1,6,6-trimethyl-8,9-dihydro-7H-naphtho[1,2-g][1]benzofuran-10,11-dione, one of the original anthracyclines isolated from Salvia miltiorrhiza,

inhibits β-amyloid aggregation and protects PC12 cells from β-amyloid-induced apoptosis.

https://www.bocsci.com/nvp-acc789-cas-300842-64-2-item-178779.htmlhttps://www.bocsci.com/ramucirumab-cas-947687-13-0-item-185679.htmlhttps://www.bocsci.com/sunitinib-cas-557795-19-4-item-186154.htmlhttps://www.bocsci.com/tanshinone-iia-cas-568-72-9-item-188817.html

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Aflibercept - CAS 862111-32-8



Description: Aflibercept is a recombinant fusion protein and acts as a VEGF inhibitor. Aflibercept is used for the treatment of wet macular degeneration and metastatic colorectal cancer.

PD173074 - CAS 219580-11-7



Description: PD173074 is a small-molecule FGFR3-selective tyrosine kinase inhibitor (TKI), as a therapeutic modality using eight UC cell lines. PD173074 suppressed cell proliferation remarkably

in two cell lines, namely, UM-UC-14 and MGHU3, which expressed mutated FGFR3 protein. Cell

cycle analysis revealed the growth inhibitory effect of PD173074 was associated with arrest at

G(1)-S transition in a dose-depending manner. In the mouse xenograft models using

subcutaneously transplanted UM-UC-14 and MGHU3, orally administered PD173074 suppressed

tumor growth and induced apoptotic changes comparable with the results of our in vitro assay.

These findings elucidated the effectiveness of molecular targeted approach for bladder UC

harboring FGFR3 mutations and the potential utility to decrease the intravesical recurrence of

nonmuscle invasive bladder UC after transurethral surgical resection.

R916562 - CAS 1037798-41-6


Molecular Weight: 536.09 Molecular Formula: C26H30ClN9S

Description: R916562, a diaminotriazole compound, is a potential and selective Axl/VEGF-R2 dual inhibitor with IC50s of 136 and 24 nM, respectively. R916562 showed activity comparable to the

clinically approved tyrosine kinase inhibitor Sunitinib in mouse tumor xenograft models and the

corneal micropocket angiogenesis model.

Anlotinib Dihydrochloride - CAS 1360460-82-7


Molecular Weight: 480.36 Molecular Formula: C23H22FN3O3.2ClH

Description: Anlotinib Dihydrochloride is a novel multi-target tyrosine kinase inhibitor with potential antineoplastic and anti-angiogenic activities, which was designed to primarily inhibit

VEGFR2/3, FGFR1-4, PDGFRα/β, c-Kit, and Ret.

https://www.bocsci.com/aflibercept-cas-862111-32-8-item-244884.htmlhttps://www.bocsci.com/pd173074-cas-219580-11-7-item-263525.htmlhttps://www.bocsci.com/r916562-cas-1037798-41-6-item-267742.htmlhttps://www.bocsci.com/anlotinib-dihydrochloride-cas-1360460-82-7-item-267743.html

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BFH772 - CAS 890128-81-1



Description: BFH772, a structure analogue of BAW2881, was highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM, however, lost 500-fold potency on FLK-1, FLT-1, and FLT-4.

BFH772 inhibits the ligand induced autophosphorylation of RET, PDGFR, and KIT kinases, with IC50

values ranging between 30 and 160 nM.

Ningetinib - CAS 1394820-69-9



Description: Ningetinib is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and

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KRN633 - CAS 286370-15-8



Description: KRN633 is a potent and selective VEGFR inhibitor. which inhibits tyrosine phosphorylation of VEGFR-2 (IC50 = 1.16 nmol/L) in human umbilical vein endothelial cells.

Selectivity profiling with recombinant tyrosine kinases showed that KRN633 is highly selective for

VEGFR-1, -2, and -3. KRN633 inhibits tumor growth in several in vivo tumor xenograft models with

diverse tissue origins, including lung, colon, and prostate, in athymic mice and rats. KRN633 also

causes the regression of some well-established tumors and those that had regrown after the

cessation of treatment. KRN633 was well tolerated and had no significant effects on body weight

or the general health of the animals. KRN633 might be useful in the treatment of solid tumors and

other diseases that depend on pathologic angiogenesis.

LY2784544 - CAS 1229236-86-5


Molecular Weight: 469.949 Molecular Formula: C23H25ClFN7O

Description: Gandotinib is a potent and selective JAK inhibitor, which effectively inhibited JAK2V617F-driven signaling and cell proliferation in Ba/F3 cells (IC50=20 and 55 nM, respectively).

RAF265 - CAS 927880-90-8



Description: RAF265 is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM.

Cabozantinib - CAS 849217-68-1



Description: Cabozantinib is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM

and 7 nM, respectively.

https://www.bocsci.com/krn633-cas-286370-15-8-item-84-286440.htmlhttps://www.bocsci.com/ly2784544-cas-1229236-86-5-item-286443.htmlhttps://www.bocsci.com/raf265-cas-927880-90-8-item-286688.htmlhttps://www.bocsci.com/cabozantinib-cas-849217-68-1-item-84-307706.html

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SU5408 - CAS 15966-93-5



Description: A potent, selective and cell-permeable inhibitor of VEGFR2 kinase(IC50= 70 nM) with little or no effect against receptors for platelet-derived growth factor, epidermal growth factor, or

insulin-like growth factor (IC50 > 100 µM).

SU11652 - CAS 326914-10-7



Description: SU11652 is a cell-permeable and sunitinib-like inhibitor of tyrosine kinase receptor (RTK) and angiogenesis with antineoplastic property. It selectively inhibits PDGFR-β, VEGFR2,

FGFR1, FLT3 (IC50 values of 3, 27, 170 and 1.5 nM, respectively) and Kit family members (IC50=~10-

500 nM).

Vatalanib - CAS 212141-54-3


Molecular Weight: 346.81 Molecular Formula: C20H15ClN4

Description: Vatalanib, also called as PTK 787 or CGP 797870, is a small molecule that interacts reversibly and competitively at the ATP-binding site of the receptor tyrosine kinase domain to

inhibit autophosphorylation. It targets all known VEGFR tyrosine kinases, th

Vandetanib - CAS 443913-73-3


Molecular Weight: 475.35 Molecular Formula: C22H24BrFN4O2

Description: Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM.

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Tyrphostin 9 - CAS 10537-47-0



Description: Tyrphostin 9 is firstly designed as an EGFR inhibitor with IC50 of 460 μM, but is also found to be more potent to PDGFR with IC50 of 0.5 μM.

PP121 - CAS 1092788-83-4



Description: PP121 is a multitargeted dual receptor tyrosine kinases inhibitor. PP121 blocks the proliferation of tumor cells by direct inhibition of oncogenic tyrosine kinases and

phosphatidylinositol-3-OH kinases.

DMH4 - CAS 515880-75-8



Description: DMH4 is a selective VEGFR-2 inhibitor (IC50 values are 161, 3558, 8038 and > 30000 nM for VEGFR-2, BMPR-I, AMPK and TGFβR-I, respectively) with antiangiogenic activity in vitro

and in vivo.

BMS-6690514 - CAS 859853-30-8



Description: BMS-690514 is a potent inhibitor of human epidermal growth factor receptor (HER) 1 (EGFR), 2, and 4, and vascular endothelial growth factor receptors (VEGFR) 1-3. BMS-690514 is

currently under investigation as an oral agent for the treatment of solid tumors. The preclinical

ADME properties of BMS-690514 suggest good oral bioavailability in humans and metabolism by

multiple pathways including oxidation and glucuronidation.

https://www.bocsci.com/https://www.bocsci.com/tyrphostin-9-cas-10537-47-0-item-84-358320.htmlhttps://www.bocsci.com/pp121-cas-1092788-83-4-item-358783.htmlhttps://www.bocsci.com/dmh4-cas-515880-75-8-item-373940.htmlhttps://www.bocsci.com/bms-6690514-cas-859853-30-8-item-385098.html

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Orantinib - CAS 252916-29-3



Description: TSU-68 (SU6668; Orantinib) is a novel multiple receptor tyrosine kinase inhibitor with IC50 of 2.1 μM, 8 nM and 1.2 μM for VEGF-R1, PDGF-Rβ and FGF-R1, respectively; has greatest

potency against PDGFR autophosphorylation.

Tivozanib - CAS 475108-18-0



Description: Tivozanib is an orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplastic activities.

Tivozanib binds to and inhibits VEGFRs 1, 2 and 3, which may result in the inhibition of endothelial

cell migration and proliferation, inhibition of tumor angiogenesis and tumor cell death. VEGFR

tyrosine kinases, frequently overexpressed by a variety of tumor cell types, play a key role in

angiogenesis. Check for active clinical trials or closed clinical trials using this agent.

ZM306416 - CAS 690206-97-4


Molecular Weight: 333.74 Molecular Formula: C16H13ClFN3O2

Description: ZM306416 is a vascular endothelial growth factor receptor (VEGFR) antagonist.

PF-03814735 - CAS 942487-16-3



Description: PF-03814735 is an orally bioavailable, ATP-competitive, reversible small-molecule Aurora kinase inhibitor with potential antineoplastic activity. Aurora kinase inhibitor PF-03814735

binds to and inhibits Aurora kinases A and B, which may result in the inhibition of cellular division

and proliferation in tumor cells that overexpress these kinases. Aurora kinases are serine-

threonine kinases that play essential roles in mitotic checkpoint control during mitosis.

https://www.bocsci.com/orantinib-cas-252916-29-3-item-409435.htmlhttps://www.bocsci.com/tivozanib-cas-475108-18-0-item-84-413727.htmlhttps://www.bocsci.com/zm306416-cas-690206-97-4-item-418967.htmlhttps://www.bocsci.com/pf-03814735-cas-942487-16-3-item-428251.html

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SU1498 - CAS 168835-82-3



Description: SU1498 is a selective inhibitor of the receptor tyrosine kinase VEGF receptor 2 (VEGFR2, aka FLK1; IC50 = 700 nM), and inhibits Flk-1 with an IC50 of value of 700 nM.

TG 100572 - CAS 867334-05-2



Description: TG 100572 is a multi-targeted kinase inhibitor that inhibits select growth factor receptor tyrosine kinases and Src familt kinases.

TG 100801 - CAS 867331-82-6



Description: TG 100801 is the prodrug of TG 100572, which is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kinases. It is currently in a

clinical trial as a first in class, VEGFr2 targeting, topically applied compound for the treatment of

AMD. It is a new drug that inhibits ocular angiogenesis, vascular leak, and inflammation in

laboratory studies.

CGP60474 - CAS 164658-13-3


Molecular Weight: 355.82 Molecular Formula: C18H18ClN5O

Description: CGP60474 is a promising inhibitor of PKC with a high degree of selectivity versus other serine/threonine and tyrosine kinases and show competitive kinetics relative to ATP.

https://www.bocsci.com/su1498-cas-168835-82-3-item-428540.htmlhttps://www.bocsci.com/tg-100572-cas-867334-05-2-item-429717.htmlhttps://www.bocsci.com/tg-100801-cas-867331-82-6-item-429718.htmlhttps://www.bocsci.com/cgp60474-cas-164658-13-3-item-430557.html

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SU14813 - CAS 627908-92-3



Description: SU14813 is an oral, multitargeted tyrosine kinase inhibitor (TKI) targeting vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR),

KIT, and fms-like tyrosine kinase 3 (FLT-3) (1). SU14813 was developed as a next-generation TKI

agent following sunitinib (SU11248) designed to demonstrate optimized pharmacokinetic (PK) and

tolerability profiles. SU14813 demonstrated broad and potent antitumor activity equivalent to that

of sunitinib, which resulted in tumor regression, growth arrest, growth delay, and prolonged

survival in established xenograft cancer models in mice.

Toceranib - CAS 356068-94-5



Description: Toceranib (CAS 356068-94-5) is a potent ATP-competitive PDGFR and VEGFR inhibitor (Ki = 5 and 6 nM, respectively); inhibits phosphorylation of c-Kit and suppresses the

growth of mast cell lines expressing mutant Kit, inducing cell cycle arrest and apoptosis. Also

inhibits FGFR1 (Ki = 0.5 μM). Effective in vivo.

TG 100801 Hydrochloride - CAS 1018069-81-2


Molecular Weight: 616.54 Molecular Formula: C33H31Cl2N5O3

Description: TG 100801 is the prodrug of TG 100572, which is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kinases with IC50 values of

2/7/2/1/0.5 nM or VEGFR1/VEGFR2/FGFR1/Src/Fy

Lucitanib - CAS 1058137-23-7



Description: Lucitanib, also known as E-3810, is a novel dual inhibitor targeting human vascular endothelial growth factor receptors (VEGFRs) and fibroblast growth factor receptors (FGFRs) with

antiangiogenic activity. VEGFR/FGFR dual kinase inhibitor E-3810 inhibits VEGFR-1, -2, -3 and

FGFR-1, -2 kinases in the nM range, which may result in the inhibition of tumor angiogenesis and

tumor cell proliferation, and the induction of tumor cell death. Both VEGFRs and FGFRs belong to

the family of receptor tyrosine kinases that may be upregulated in various tumor cell types.

https://www.bocsci.com/su14813-cas-627908-92-3-item-431172.htmlhttps://www.bocsci.com/toceranib-cas-356068-94-5-item-455463.htmlhttps://www.bocsci.com/tg-100801-hydrochloride-cas-1018069-81-2-item-84-456447.htmlhttps://www.bocsci.com/lucitanib-cas-1058137-23-7-item-456732.html

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Cabozantinib malate (XL184) - CAS 1140909-48-3


Molecular Weight: 635.59 Molecular Formula: C28H24FN3O5.C4H6O5

Description: Cabozantinib malate is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM,

4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively.

EG00229 - CAS 1210945-69-9


Molecular Weight: 611.6 Molecular Formula: C19H20F3N7O7S3

Description: EG00229 is a small molecule inhibitor of neuropilin-1(Nrp1) with an IC50 of 3μM. EG00229 has been reported to inhibit VEGF-A binding to PAE/NRP1 in the Nrp1and bt-VEGF-A

binding to purified Nrp1 b1 domain in a cell-free assay with an IC50 value of 8μM and 3μM,

respectively. In addition, EG00229 has also shown the inhibition of VEGF-A binding to VEGFR2,

VEGFR1 and Nrp1 in human umbilical vein endothelial cells (HUVECs) in a dose-dependent manner

with an IC50 value of 23μM [1]. Besides, EG00229 has been revealed to prevent tuftsin binding to

the Nrp1 which is at the cell surface. Moreover, EG00229 has been noted to suppress the anti-

inflammatory M2 shift in microglia induced by tuftsin and thus potently prevent tuftsin’s action.

Apatinib - CAS 1218779-75-9



Description: Apatinib mesylate is an orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. Apatinib selectively binds to

and inhibits vascular endothelial growth factor receptor 2, which may inhibit VEGF-stimulated

endothelial cell migration and proliferation and decrease tumor microvessel density. In addition,

this agent mildly inhibits c-Kit and c-SRC tyrosine kinases.

ENMD-2076 L-(+)-Tartaric acid - CAS 1291074-87-7



Description: ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076, selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold more selective for Aurora A than

Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2

https://www.bocsci.com/cabozantinib-malate-xl184-cas-1140909-48-3-item-457054.htmlhttps://www.bocsci.com/eg00229-cas-1210945-69-9-item-84-457636.htmlhttps://www.bocsci.com/apatinib-cas-1218779-75-9-item-84-457664.htmlhttps://www.bocsci.com/enmd-2076-l-tartaric-acid-cas-1291074-87-7-item-457865.html

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XL-647 - CAS 781613-23-8


Molecular Weight: 491.39 Molecular Formula: C24H25Cl2FN4O2

Description: XL647 is an orally bioavailable small-molecule receptor tyrosine kinase inhibitor with potential antineoplastic activity. It inhibits EGFR, HER2, VEGFR and EphB4 kinase.

Regorafenib Hydrochloride - CAS 835621-07-3


Molecular Weight: 519.28 Molecular Formula: C21H16Cl2F4N4O3

Description: Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1.

SU14813 maleate - CAS 849643-15-8



Description: SU14813 maleate is an oral, multitargeted tyrosine kinase inhibitor (TKI) targeting vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors

(PDGFR), Kit, and fms-like tyrosine kinase 3 (FLT-3). It was developed as a next-generation TKI

agent following sunitinib (SU11248) designed to demonstrate optimized pharmacokinetic (PK) and

tolerability profiles. It demonstrated broad and potent antitumor activity equivalent to that of

sunitinib, which resulted in tumor regression, growth arrest, growth delay, and prolonged survival

in established xenograft cancer models in mice.

Cediranib maleate - CAS 857036-77-2



Description: Cediranib maleate is a highly potent VEGFR (KDR) inhibitor with IC50 of

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TG 100572 Hydrochloride - CAS 867331-64-4


Molecular Weight: 512.43 Molecular Formula: C26H27Cl2N5O2

Description: TG 100572 is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kinases for VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse.

ZK-261991 - CAS 886563-25-3



Description: ZK-261991 is an orally active VEGFR tyrosine kinase inhibitor with an IC50 of 5 nM for VEGFR2. The high efficacy, including tumour regression in established tumours, combined with its

low toxicity recommends ZK 261991 for development as a drug for the therapy of solid tumours

also in combination with other chemotherapeutics.

Golvatinib - CAS 928037-13-2



Description: golvatinib (also known as E7050) is an orally bioavailable dual kinase inhibitor of c-Met (hepatocyte growth factor receptor) and VEGFR-2 (vascular endothelial growth factor

receptor-2) tyrosine kinases with potential antineoplastic activity. c-Met/VEGFR kinase inhibitor

E7050 binds to and inhibits the activities of both c-Met and VEGFR-2, which may inhibit tumor cell

growth and survival of tumor cells that overexpress these receptor tyrosine kinases. c-Met and

VEGFR-2 are upregulated in a variety of various tumor cell types and play important roles in tumor

cell growth, migration and angiogenesis.

Axitinib - CAS 319460-85-0


Molecular Weight: 386.47 Molecular Formula: C22H18N4OS

Description: axitinib is an orally bioavailable tyrosine kinase inhibitor. Axitinib inhibits the proangiogenic cytokines vascular endothelial growth factor (VEGF) and platelet-derived growth

factor receptor (PDGF), thereby exerting an anti-angiogenic effect.

https://www.bocsci.com/tg-100572-hydrochloride-cas-867331-64-4-item-460028.htmlhttps://www.bocsci.com/zk-261991-cas-886563-25-3-item-460234.htmlhttps://www.bocsci.com/golvatinib-cas-928037-13-2-item-460626.htmlhttps://www.bocsci.com/axitinib-cas-319460-85-0-item-84-461979.html

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XL999 - CAS 705946-27-6



Description: XL999, a Spectrum Selective Kinase Inhibitor(TM) (SSKIs), is a potent inhibitor of key RTKs implicated in the development and maintenance of tumor vasculature and in the

proliferation of some tumor cells. It inhibits the FGFR, VEGFR and PDGFR RTKs and exhibited

excellent activity in target-specific cellular functional assays. In addition, XL999 is a potent

inhibitor of FLT3, an important driver of leukemia cell proliferation in some patients with acute

myelogenous leukemia (AML). In several preclinical models of human tumors, including breast,

lung, colon and prostate cancer, XL999 demonstrated potent inhibition of tumor growth, and also

caused regression of large well-established tumors. Phase I studies of XL999 established a

maximum tolerated dose and showed evidence of tumor responses.

JI-101 - CAS 900573-88-8


Molecular Weight: 466.339 Molecular Formula: C22H20BrN5O2

Description: JI-101 is an orally active inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor beta (PDGFRb), and the ephrin B4 receptor B4

(EphB4) with potential antiangiogenic and antineoplastic activities. Angiogenesis inhibitor JI-101

binds to and inhibits VEGFR2, PDGFRb and EphB4, which may inhibit tumor angiogenesis and, so,

cellular proliferation in tumor cells overexpressing VEGFR2, PDGFRb and EphB4. The receptor

tyrosine kinases VEGFR2, PDGFRb and EphB4 may be overexpressed in a number of different

cancer cell types and may play crucial roles in tumor angiogenesis.

SKLB610 - CAS 1125780-41-7



Description: SKLB610 is a VEGFR inhibitor that potently suppresses human tumor angiogenesis. SKLB610 inhibited angiogenesis-related tyrosine kinase VEGFR2, fibroblast growth factor

receptor 2 (FGFR2) and platelet-derived growth factor receptor (PDGFR) at rate of 97%, 65% and

55%, respectively, at concentration of 10μM in biochemical kinase assays. SKLB610 exhibited its

antitumor activity as a multi-targeted inhibitor with more potent inhibition of VEGFR2 activity. Its

potential to be a candidate of anticancer agent is worth being further investigated.

https://www.bocsci.com/xl999-cas-705946-27-6-item-462245.htmlhttps://www.bocsci.com/ji-101-cas-900573-88-8-item-462546.htmlhttps://www.bocsci.com/sklb610-cas-1125780-41-7-item-462581.html

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SKLB1002 - CAS 1225451-84-2



Description: SKLB1002 is a new potent VEGFR2 inhibitor, which could significantly inhibit HUVEC proliferation, migration, invasion, and tube formation. In vivo zebrafish model experiments

showed that SKLB1002 remarkably blocked the formation of intersegmental vessels in zebrafish

embryos. SKLB1002 inhibits angiogenesis and may be a potential drug candidate in anticancer

therapy.

Ilorasertib - CAS 1227939-82-3


Molecular Weight: 488.541 Molecular Formula: C25H21FN6O2S

Description: Ilorasertib, also known as ABT-348, is a novel, potent and orally bioavailable inhibitor of the Aurora kinases as well as the VEGF and PDGF families of receptor tyrosine kinases and is

currently in Phase I clinical trials. ABT-348 has nanomolar potency (IC50) for inhibiting binding

and cellular auto-phosphorylation of Aurora B (7 and 13 nM), C (1 and 13 nM) and A (120 and 189

nM). These results provide the rationale for clinical assessment of ABT-348 as a therapeutic agent

in the treatment of cancer.

R1530 - CAS 882531-87-5


Molecular Weight: 356.78136 Molecular Formula: C18H14ClFN4O

Description: R1530 is a pyrazolobenzodiazepine small molecule with potential antiangiogenesis and antineoplastic activities. R1530 is also a mitosis-angiogenesis inhibitor (MAI) that inhibits

multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial growth

factor receptor (VEGFR)-1, -2, -3, platelet-derived growth factor receptor (PDGFR) beta‚ FMS-like

tyrosine kinase (Flt)-3, and fibroblast growth factor receptor (FGFR) -1, -2. In addition, this agents

exhibits anti-proliferative activity by initiating mitotic arrest and inducing apoptosis.

https://www.bocsci.com/sklb1002-cas-1225451-84-2-item-84-462582.htmlhttps://www.bocsci.com/ilorasertib-cas-1227939-82-3-item-462639.htmlhttps://www.bocsci.com/r1530-cas-882531-87-5-item-84-462772.html

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TAK-593 - CAS 1005780-62-0



Description: TAK-593 is an oral formulation containing a small-molecule receptor tyrosine kinase inhibitor of both vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth

factor receptor (PDGFR) with potential antineoplastic activity. TAK-593 selectively binds to and

inhibits VEGFR and PDGFR, which may result in the inhibition of angiogenesis and tumor cell

proliferation. Check for active clinical trials or closed clinical trials using this agent.

Altiratinib - CAS 1345847-93-9



Description: Altiratinib, also known as DCC-270, DP-5164, is an oral, selective and highly potent inhibitor of MET, TIE2, VEGFR2 and TRK kinases with potential anticancer activity. DCC-2701

effectively reduces tumor burden in vivo and blocks c-MET pTyr(1349)-mediated signaling, cell

growth and migration as compared with a HGF antagonist in vitro. Importantly, DCC-2701's anti-

proliferative activity was dependent on c-MET activation induced by stromal human fibroblasts

and to a lesser extent exogenous HGF. DCC-2701 may be superior to HGF antagonists that are in

clinical trials and that pTyr(1349) levels might be a good indicator of c-MET activation and likely

response to targeted therapy as a result of signals from the microenvironment.

2,4-Pyrimidinediamine with linker - CAS 1430089-64-7



Description: 2,4-Pyrimidinediamine with linker is a patent compound in WO2013055780A1, Page 71; multikinase inhibitor and has a -NH2 terminal linker for further synthesis.

https://www.bocsci.com/tak-593-cas-1005780-62-0-item-462796.htmlhttps://www.bocsci.com/altiratinib-cas-1345847-93-9-item-463181.htmlhttps://www.bocsci.com/2-4-pyrimidinediamine-with-linker-cas-1430089-64-7-item-84-463236.html

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WHI-P180 hydrochloride - CAS 153437-55-9



Description: WHI-P180 moderately inhibited ABCG2 function, exhibiting weak phototoxicity. The elimination half-life of WHI-P180 in CD-1 mice (BALB/ c mice) following i.v., i.p., or p.o.

administration was less than 10 min. Systemic clearance of WHI-P180 was 6742 mL/h/kg in CD-I

mice and 8188 mL/h/kg in BALB/c mice. Notably, WHI-P180, when administered in two consecutive

nontoxic i.p. bolus doses of 25 mg/kg, inhibited IgE/antigen-induced vascular hyperpermeability

in a well-characterized murine model of passive cutaneous anaphylaxis.

Vandetanib hydrochloride - CAS 524722-52-9


Molecular Weight: 511.81 Molecular Formula: C22H25BrClFN4O2

Description: Vandetanib hydrochloride is an anti-cancer drug that is used for the treatment of certain tumours of thethyroid gland. It acts as a kinase inhibitor of a number of cell receptors,

mainly the vascular endothelial growth factor receptor (VEGFR), the epidermal growth factor

receptor (EGFR), and the RET-tyrosine kinase.

AST 487 - CAS 630124-46-8



Description: AST487 is a Ret kinase inhibitor/FLT3 inhibitor, which displays high selectivity and potency toward FLT3 as a molecular target, and which could potentially be used to override drug

resistance in AML. It induced a dose-dependent growth inhibition of xenografts of NIH3T3 cells

expressing oncogenic RET, and of the MTC cell line TT in nude mice.It also inhibited calcitonin

gene expression in vitro in TT cells, in part, through decreased gene transcription.

SAR131675 - CAS 1433953-83-3



Description: SAR131675 dose dependently inhibits the proliferation of primary human lymphatic cells, induced by the VEGFR-3 ligands VEGFC and VEGFD, with an IC50 of about 20 nM.

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Regorafenib monohydrate - CAS 1019206-88-2



Description: Regorafenib monohydrate is a multitargetedinhibitor of tyrosine kinase with IC50 values of 13nM, 4.2nM, 46nM, 2.5nM, 28nM, 19nM, 202nM, 22nM, 7nM, 1.5nM and 311nM, respectively

for VEGFR-1, mVEGFR-2, mVEGFR-3, Raf-1, BRAF WT, BRAFV600E, FGFR-1, PDGFR-β, c-KIT, RET

and TIE2.

ZM323881 hydrochloride - CAS 193000-39-4


Molecular Weight: 411.86 Molecular Formula: C22H19ClFN3O2

Description: Potent and selective inhibitor of VEGFR2 (IC50: 2 nM for VEGFR2 vs >50 mM for VEGFR1 respectively)

ZM323881 - CAS 193001-14-8



Description: ZM323881 inhibits VEGF-A, EGF and bFEF induced HUVEC cell proliferation with IC50 of 8 nM, 1.9 μM and 1.6 μM, respectively. ZM323881 (10 nM) abolishes VEGF-A-mediated increases

in vascular permeability in perfused mesenteric microvessels in male leopard. ZM323881 (10 nM)

blocks the increase in intensity of the VEGF-R2 band in the lung of male leopard frogs. M323881 (1

μM) blocks activation of extracellular regulated-kinase, p38, Akt, and endothelial nitric oxide

synthetase (eNOS) by VEGF, but did not inhibit p38 activation by the VEGFR-1-specific ligand,

placental growth factor (PIGF) in human aortic endothelial cells (HAECs). ZM323881 (1 μM) also

perturbes VEGF-induced membrane extension, cell migration, and tube formation by HAECs.

ZM323881 (1 μM) reverses VEGF-stimulated phosphorylation of CrkII and its Src homology 2 (SH2)-

binding protein p130Cas, which are known to play a pivotal role in regulating endothelial cell

migration. ZM323881 (10 nM) completely blocks VEGF-induced VEGF promoter activity in SCC-9

cells. ZM323881 (10 nM) blocks VEGF stimulated Hif-1α protein accumulation in SCC-9 cells.

ZM323881 (10 nM) blocks VEGF-induced Rac1 activation at 30 min in HUVECs. ZM323881 (10 nM)

prevents Vav2 tyrosine phosphorylation in response to VEGF in HUVECs.

https://www.bocsci.com/regorafenib-monohydrate-cas-1019206-88-2-item-84-463493.htmlhttps://www.bocsci.com/zm323881-hydrochloride-cas-193000-39-4-item-84-463579.htmlhttps://www.bocsci.com/zm323881-cas-193001-14-8-item-84-463580.html

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Vandetanib trifluoroacetate - CAS 338992-53-3


Molecular Weight: 589.38 Molecular Formula: C24H25BrF4N4O4

Description: Vandetanib is an anti-cancer drug that is used for the treatment of certain tumours of thethyroid gland. It acts as a kinase inhibitor of a number of cell receptors, mainly the vascular

endothelial growth factor receptor (VEGFR), the epidermal growth factor receptor (EGFR), and the

RET-tyrosine kinase.

AZD2932 - CAS 883986-34-3



Description: AZD2932 is a new quinazoline ether inhibitor and is a high affinity inhibitor of VEFGR-2 and PDGFR. It has a balanced ~1:1 ratio of activity vs both VEGFR-2 and PDGFRβ. It is also active

on c-Kit and FLT3 with good selectivity on a panel of kinases.

ACTB-1003 - CAS 939805-30-8



Description: ACTB-1003 is an oral kinase inhibitor with multiple modes of action, targeting cancer mutations via FGFR inhibition FGFR1, angiogenesis through inhibition of VEGFR2, Tie-2, and

induces apoptosis likely by targeting RSK and p70S6K. It is highly active with dose-dependent

tumor growth inhibition in cell lines with FGFR genetic alterations - OPM2 human multiple

myeloma and the murine leukemia Ba/F3-TEL-FGFR1.

Fruquintinib - CAS 1194506-26-7



Description: Fruquintinib, also known as HMPL-013, is an orally available, small molecule inhibitor of vascular endothelial growth factor receptors (VEGFRs), with potential anti-angiogenic and

antineoplastic activities.

https://www.bocsci.com/vandetanib-trifluoroacetate-cas-338992-53-3-item-84-463630.htmlhttps://www.bocsci.com/azd2932-cas-883986-34-3-item-463669.htmlhttps://www.bocsci.com/actb-1003-cas-939805-30-8-item-463692.htmlhttps://www.bocsci.com/fruquintinib-cas-1194506-26-7-item-470819.html

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Anlotinib - CAS 1058156-90-3



Description: Anlotibib is a multi-targetes kinase inhibitor of receptor tyrosine and could effectively resist the formation of new angiogenesis and is under Phase III trial for exploring the

effectiveness and safety of andvanced non-small cell lung cancer by Chiatai T

SCR-1481B1 - CAS 1174161-86-4


Molecular Weight: 699.98 Molecular Formula: C28H29ClF2N5O10P

Description: SCR-1481B1, also known as c-Met inhibitor 2, is an effective inhibitor of MET kinase so that probably has anti-tumor activity. It is also found to be an inhibitor of VEGFR. IC50: 1.7 nM for

MET kinase.

Flumatinib - CAS 895519-90-1



Description: Flumatinib is a multi-kinase inhibitor of c-Abl, PDGFRβ and c-Kit with IC50 values of 1.2 nM, 307.6 nM and 2662 nM respectively. It can predominantly inhibit the autophosphorylation

of Bcr-Abl in K562 cell in vitro. It can inhibit the phosphorylation of c-Kit in Mo7e cell and the

phosphorylation of PDGFR in Swiss3T3 cell in higher concentration. It has no or little effect on

other tyrosine kinase including EGFR、KDR、c-Src andHER2. It can reduce the expression of C-

MYC, HIF-1 α and VEGF in U266 cell line in a time- and dose-dependent manners. It effectively

overcame the drug resistance of certain KIT mutants with activation loop mutations. It was

developed by Jiangsu Hansoh Pharmaceutical Co., Ltd. and is currently in Phase III clinical trials

in China for the treatment of chronic myelogenous leukemia (CML).

https://www.bocsci.com/anlotinib-cas-1058156-90-3-item-474328.htmlhttps://www.bocsci.com/scr-1481b1-cas-1174161-86-4-item-474369.htmlhttps://www.bocsci.com/flumatinib-cas-895519-90-1-item-474894.html

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TAS-115 - CAS 1190836-34-0


Molecular Weight: 518.56 Molecular Formula: C27H23FN4O4S

Description: This active molecular is a c-MET and VEGFR inhibitor which is selective and specific in vitro. In vivo studies, TAS-115 suppressed the progression of MET-inactivated tumor completely

through blocking angiogenesis without toxicity and it also induced marked tumor shrinkage and

prolonged survival in animal model. In Dec 2013, Phase-I development was ongoing in Japan. In

Dec 2014, Taiho Pharmaceutical completed a phase I trial for Solid tumours in Japan. In Apr 2016,

preclinical data was presented.

ARQ 736 disodium salt - CAS 1228237-57-7


Molecular Weight: 674.54 Molecular Formula: C25H25N8Na2O8PS

Description: This active molecular is a Proto oncogene protein b raf and Vascular endothelial growth factor a inhibitor originated by ArQule. ARQ 736 is effective in killing cancer cell lines that

harboring at least one mutated b raf allele. The b raf protein is really a very important signaling

molecule in the MAPK (mitogen activated protein kinase) signaling pathway and it relates to

pathogenesis of variety kinds of cancer. In Mar 2014, Phase-I for Solid tumours (late-stage disease)

was discontinued in USA.

BRN-103 - CAS 1346265-80-2


Molecular Weight: 420.93 Molecular Formula: C24H25ClN4O

Description: BRN-103 can suppress the phosphorylation of vascular endothelial growth factor (VEGF) receptor 2. It can also inhibit the activations of AKT and eNOS. These results show that

BRN-103 inhibits VEGF-mediated angiogenesis signaling in human endothelial cells.

JNJ 17029259 - CAS 314267-57-7



Description: JNJ 17029259 is an selective, nanomolar inhibitors of the vascular endothelial growth factor receptor-2 (VEGF-R2), blocks VEGF-stimulated mitogen-activated protein kinase signaling,

proliferation/migration.

https://www.bocsci.com/tas-115-cas-1190836-34-0-item-475134.htmlhttps://www.bocsci.com/arq-736-disodium-salt-cas-1228237-57-7-item-475181.htmlhttps://www.bocsci.com/brn-103-cas-1346265-80-2-item-475331.htmlhttps://www.bocsci.com/jnj-17029259-cas-314267-57-7-item-475639.html

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AG28262 - CAS 638216-89-4



Description: AG28262 is a bio-active chemical compound. It is a VEFG-r2 inhibitor and could cause an increase in serum ALT, due in part to both gene up-regulation.

BAW2881 - CAS 861875-60-7



Description: BAW 2881 is a VEGFR (vascular endothelial growth factor receptor) inhibitor (IC50 = 0.82, 0.037, and 0.42 µM for VEGFR1, 2, and 3, respectively).It can inhibit proliferation, migration,

and tube formation by human umbilical vein endothelial cells and lymphatic endothelial cells in

vitro.

https://www.bocsci.com/ag28262-cas-638216-89-4-item-476068.htmlhttps://www.bocsci.com/baw2881-cas-861875-60-7-item-476680.html

Documents

VEGFR Inhibitors (inhibitors, agonists and modulators)...Tel: 1-631-504-6093 Fax: 1-631-614-7828 E-mail: [email protected] 45-16 Ramsey Road Shirley, NY 11967, USA VEGFR Inhibitors (inhibitors,