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Golvatinib (E7050)

Golvatinib (E7050) structure

CAS No:
928037-13-2
Formula:
C33H37F2N7O4
Chemical 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)-
Categories:
Biochemical Engineering > Inhibitors

Description

E-7050 is a potent dual inhibitor of both c-Met and VEGFR2 kinases with IC50s of 14 and 16 nM, respectively.

Golvatinib is an aromatic ether.|Golvatinib has been investigated for the treatment of Platinum-Resistant Squamous Cell Carcinoma of the Head and Neck.|Golvatinib 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 tumor cell types and play important roles in tumor cell growth, migration and angiogenesis.

Golvatinib (E7050) Basic Attributes

Molecular Weight：

633.6881864

Exact Mass：

633.287537

UNII：

516Z3YP58E

DSSTox ID：

DTXSID40239155

NCI Thesaurus Code：

C82363

Characteristics

PSA：

119

XLogP3：

4.1

Density：

1.4±0.1 g/cm3

Flash Point：

478.5±34.3 °C

Refractive Index：

1.671

Drug Information

MeSH Entry Terms：

E 7050

Golvatinib (E7050) Use and Manufacturing

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.

Computed Properties

Molecular Weight:633.7
XLogP3:4.1
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:9
Rotatable Bond Count:8
Exact Mass:633.28750901
Monoisotopic Mass:633.28750901
Topological Polar Surface Area:119
Heavy Atom Count:46
Complexity:1060
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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Golvatinib(E7050)

CAS No.: 928037-13-2

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