BI-0474 (BI 0474)

Chemical Structure : BI-0474

CAS No.: 2750570-55-7

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货号: PC-49406Not For Human Use, Lab Use Only.

BI-0474 (BI 0474) is a potent, in vivo active KRAS G12C inhibitor with IC50 of 7.0 nM in GDP-KRAS::SOS1 protein-protein interaction assay.

规格	价格	库存
1 mg	￥1980	In stock
5 mg	￥3980	In stock
10 mg	￥5880	In stock
25 mg	￥9880	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

BI-0474 (BI 0474) is a potent, in vivo active KRAS G12C inhibitor with IC50 of 7.0 nM in GDP-KRAS::SOS1 protein-protein interaction assay.
BI-0474 binds reversibly to the switch II pocket.
BI-0474 showed potent antiproliferative activity (IC50=26 nM) on NCI-H358 cells carrying a G12C mutation, with no antiproliferative effect on cells carrying a KRASG12D mutation.
BI-0474 already showed a slightly higher second-order rate and lower KI, comparable kinact and IC50 in the biochemical assay, compared with AMG-510.
BI-0474 (40 mg/kg, i.p,) shows efficacy in an NCI-H358 non-small cell lung cancer xenograft model.

物理化学性质&存储条件

分子量	587.747
分子式	C30H37N9O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(4S)-2-Amino-4-(3-{6-[(2S)-2,4-dimethylpiperazin-1-yl]-4-[4-(prop-2-enoyl)piperazin-1-yl]pyridin-2-yl}-1,2,4-oxadiazol-5-yl)-4-methyl-4,5,6,7-tetrahydro-1-benzothiophene-3-carbonitrile

参考文献

1. Joachim Bröker, et al. J Med Chem. 2022 Oct 27. doi: 10.1021/acs.jmedchem.2c01120.

BI-0474 (BI 0474)

生物&药学活性

物理化学性质&存储条件

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BI-0474 (BI 0474)

生物&药学活性

物理化学性质&存储条件

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