The detail information for Golvatinib

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Golvatinib (E7050) Basic information

Description In vitro In vivo In vivo

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Product Name:

Golvatinib (E7050)

Synonyms:

N-[2-Fluoro-4-[[2-[[[4-(4-methylpiperazin-1-yl)piperidin-1-yl]carbonyl]amino]pyridin-4-yl]oxy];E-7050N-[2-Fluoro-4-[[2-[[[4-(4-methylpiperazin-1-yl)piperidin-1-yl]carbonyl]amino]pyridin-4-yl]oxy]phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide;E-7050;N-[2-Fluoro-4-[[2-[[[4-(4-methylpiperazin-1-yl)piperidin-1-yl]carbonyl]amino]pyridin-4-yl]oxy]phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide;Golvatinib;E-7050 (Golvatinib);Golvatinib (E7050);1,1-Cyclopropanedicarboxamide, N-[2-fluoro-4-[[2-[[[4-(4-methyl-1-piperazinyl)-1-piperidinyl]carbonyl]amino]-4-pyridinyl]oxy]phenyl]-N'-(4-fluorophenyl)-

CAS:

928037-13-2

MF:

C33H37F2N7O4

MW:

633.6881864

EINECS:

 

Product Categories:

Inhibitors

Mol File:

928037-13-2.mol

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Golvatinib (E7050) Chemical Properties

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Boiling point 

867.5±65.0 °C(Predicted)

density 

1.408

pka

12.91±0.70(Predicted)

CAS DataBase Reference

928037-13-2

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Safety Information

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MSDS Information

 

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Golvatinib (E7050) Usage And Synthesis

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Description

Golvatinib (E7050) is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM, does not inhibit bFGF-stimulated HUVEC growth (up to 1000 nM). Phase 1/2.

In vitro

In vitro studies indicate that E7050 potently inhibits phosphorylation of both c-Met and VEGFR-2. E7050 also potently represses the growth of both c-met amplified tumor cells and endothelial cells stimulated with either HGF or VEGF. E7050 circumvents resistance to all of the reversible, irreversible, and mutant-selective EGFR-TKIs induced by exogenous and/or endogenous HGF in EGFR mutant lung cancer cell lines, by blocking the Met/Gab1/PI3K/Akt pathway in vitro. E7050 also prevents the emergence of gefitinib-resistant HCC827 cells induced by continuous exposure to HGF.

In vivo

In vivo studies using E7050 shows inhibition of the phosphorylation of c-Met and VEGFR-2 in tumors, and strong inhibition of tumor growth and tumor angiogenesis in xenograft models. Treatment of some tumor lines containing c-met amplifications with high doses of E7050 (50–200 mg/kg) induces tumor regression and disappearance. In a peritoneal dissemination model, E7050 shows an antitumor effect against peritoneal tumors as well as a significant prolongation of lifespan in treated mice. In another xenograft model research, tumors produced by HGF-transfected Ma-1 (Ma-1/HGF) cells are more angiogenic than vector control tumors and shows resistance to ZD1839. E7050 alone inhibits angiogenesis and retards growth of Ma-1/HGF tumors. E7050 combined with ZD1839 induces marked regression of tumor growth.

In vivo

In vivo studies using E7050 shows inhibition of the phosphorylation of c-Met and VEGFR-2 in tumors, and strong inhibition of tumor growth and tumor angiogenesis in xenograft models. Treatment of some tumor lines containing c-met amplifications with high doses of E7050 (50–200 mg/kg) induces tumor regression and disappearance. In a peritoneal dissemination model, E7050 shows an antitumor effect against peritoneal tumors as well as a significant prolongation of lifespan in treated mice. In another xenograft model research, tumors produced by HGF-transfected Ma-1 (Ma-1/HGF) cells are more angiogenic than vector control tumors and shows resistance to ZD1839. E7050 alone inhibits angiogenesis and retards growth of Ma-1/HGF tumors. E7050 combined with ZD1839 induces marked regression of tumor growth.

Uses

E7050 is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM, respectively.

Uses

Golvatinib is a potent and orally available inhibitor of c-MET and VEGFR-2 that exhibits potential antitumor properties by suppressing the overexpression of these receptor tyrosine kinases.