A dual inhibitor of c-Met and VEGFR2; inhibits autophosphorylation of c-Met and phosphorylation of VEGFR2 (IC50s = 14 and 16 nM

Golvatinib – 1 mg

Brand:
Cayman
CAS:
928037-13-2
Storage:
-20
UN-No:
Non-Hazardous - /

Golvatinib is an orally bioavailable dual inhibitor of the receptor tyrosine kinases c-Met and VEGF receptor 2 (VEGFR2), which are involved in tumor progression.{41051} Golvatinib inhibits autophosphorylation of c-Met in MKN45 cells and phosphorylation of VEGFR2 in human umbilical vein endothelial cells (HUVECs; IC50s = 14 and 16 nM, respectively). It also inhibits proliferation of a variety of cancer cell lines and of HUVECs stimulated with hepatocyte growth factor (HGF) and VEGF but not bFGF (IC50s = 17, 84, and >1,000 nM for HGF-, VEGF-, and bFGF-stimulated HUVECs, respectively). In nude mouse xenograft models using MKN45, Hs746T, SNU-5, or EBC-1 cancer cells, golvatinib (25-200 mg/kg, daily) dose-dependently reduces tumor volume, and it increases survival in the model using MKN45 cells.  

 

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Description

A dual inhibitor of c-Met and VEGFR2; inhibits autophosphorylation of c-Met and phosphorylation of VEGFR2 (IC50s = 14 and 16 nM, respectively); inhibits proliferation in a variety of cancer cell lines; inhibits proliferation of HUVECs stimulated with HGF and VEGF but not bFGF (IC50s = 17, 84, and >1,000 nM); reduces tumor volume dose-dependently in nude mouse xenograft models using MKN45, Hs746T, SNU-5, or EBC-1 cells; increases survival of nude mice implanted with MKN45 cancer cells

Formal name: N-[2-fluoro-4-[[2-[[[4-(4-methyl-1-piperazinyl)-1-piperidinyl]carbonyl]amino]-4-pyridinyl]oxy]phenyl]-N’-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide

Synonyms:  E7050

Molecular weight: 633.7

CAS: 928037-13-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Receptor Tyrosine Kinases||Product Type|Biochemicals|Kinase Inhibitors|VEGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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