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RAF265(CHIR-265)

RAF265(CHIR-265) structure

CAS No:
927880-90-8
Formula:
C24H15F6N6O
Chemical Name:
RAF265(CHIR-265)
Synonyms:
RAF265(CHIR-265);RAF265;CHIR-265 or RAF265;1-Methyl-5-[[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]-4-pyridinyl]oxy]-N-[4-(trifluoromethyl)phenyl]-1H-benzimidazol-2-amine;1-methyl-5-(2-(5-(trifluoromethyl)-1H-imidazol-2-yl)pyridin-4-yloxy)-N-(4-(trifluoromethyl)phenyl)-1H-benzo[d]imidazol-2-amine;1-Methyl-5-[[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]-4-pyridinyl]oxy]-N-[4-(trifluoromethyl)phenyl]-1H-benzimidazol-2-amineRAF265 (CHIR-265);RAF 2651-Methyl-5-[[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]-4-pyridinyl]oxy]-N-[4-(trifluoromethyl)phenyl]-1H-benzimidazol-2-amine;1H-Benzimidazol-2-amine, 1-methyl-5-[[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]-4-pyridinyl]oxy]-N-[4-(trifluoromethyl)phenyl]-
Categories:
Biochemical Engineering > Inhibitors

Description

RAF265 is a potent RAF/VEGFR2 inhibitor.

1-methyl-5-[[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]-4-pyridinyl]oxy]-N-[4-(trifluoromethyl)phenyl]-2-benzimidazolamine is an aromatic ether.

RAF265(CHIR-265) Basic Attributes

Molecular Weight：

517.4059192

Exact Mass：

518.128967

EC Number：

-0

UNII：

8O434L3768

Characteristics

PSA：

80.6

XLogP3：

5.4

Density：

1.5±0.1 g/cm3

Boiling Point：

667.6±65.0°C at 760 mmHg

Flash Point：

357.5±34.3 °C

Refractive Index：

1.622

Drug Information

Drug Indication：

Investigated for use/treatment in melanoma.

Mechanism of Action：

CHIR-265 binds and inhibits Raf kinases, which may result in a reduction of tumor cell growth and proliferation, and tumor cell death. In addition, this agent inhibits vascular endothelial growth factor receptor type 2 (VEGFR-2), thereby disrupting tumor angiogenesis. Raf kinases are critical enzymes in the Ras/Raf/MEK/ERK signaling pathway and are frequently upregulated in neoplasms.

MeSH Entry Terms：

CHIR-265

RAF265(CHIR-265) Use and Manufacturing

RAF 265 is a multikinase inhibitor that has displayed BRAF inhibiting activity in clinical trials. It could be used in the treatment of a subpopulation of human melanoma tumors. Has cytotoxic effect of on MDA-MB-231 cells. RAF265 when used with BEZ-235 inhibited ERK, PI3K signaling that reduced growth, proliferation and development of drug resistance in human thyroid cancer cells.

Computed Properties

Molecular Weight:518.4
XLogP3:5.4
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:11
Rotatable Bond Count:5
Exact Mass:518.12897813
Monoisotopic Mass:518.12897813
Topological Polar Surface Area:80.6
Heavy Atom Count:37
Complexity:763
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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