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Chemical Structure : BI-0474
CAS No.: 2750570-55-7
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 2 mg | $398 | In stock | |
| 5 mg | $598 | In stock | |
| 10 mg | $898 | In stock | |
| 25 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 587.747 | |
| Formula | C30H37N9O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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1. Joachim Bröker, et al. J Med Chem. 2022 Oct 27. doi: 10.1021/acs.jmedchem.2c01120.
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