Chemical Structure : BI-3406
CAS No.: 2230836-55-0
货号: PC-38296Not For Human Use, Lab Use Only.
BI-3406 (BI 3406) is a highly potent and selective SOS1-KRAS interaction inhibitor with IC50 of 5 nM, binds to the catalytic domain of SOS1 with Kd of 9.7 nM.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5 mg | ¥1380 | In stock | |
10 mg | ¥2180 | In stock | |
25 mg | ¥3680 | In stock | |
50 mg | ¥5880 | In stock | |
100 mg | Get quote |
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BI-3406 (BI 3406) is a highly potent and selective SOS1-KRAS interaction inhibitor with IC50 of 5 nM, binds to the catalytic domain of SOS1 with Kd of 9.7 nM.
BI-3406 selectively disrupted the protein-protein interaction between K-RasG12C or K-RasG12D with SOS1 over SOS2, inhibited RAS-GTP levels with an IC50 of 83–231 nM in SOS1/KRAS-dependent NCI-H358 (KRAS G12C) and A549 (KRAS G12S) cell, reduces pERK levels in RAS-mutated cell lines with IC50 of 17-57 nM.
BI-3406 reduces formation of GTP-loaded RAS and limits cellular proliferation of a broad range of KRAS-driven cancers.
BI-3406 attenuates feedback reactivation induced by MEK inhibitors and enhances sensitivity of KRAS-dependent cancers to MEK inhibition.
Combined SOS1 and MEK inhibition represents a novel and effective therapeutic concept to address KRAS-driven tumors.
分子量 | 462.473 | |
分子式 | C23H25F3N4O3 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
N-[(1R)-1-[3-amino-5-(trifluoromethyl)phenyl]ethyl]-7-methoxy-2-methyl-6-[[(3S)-tetrahydro-3-furanyl]oxy]-4-quinazolinamine |
1. Hofmann MH, et al. Cancer Discov. 2021 Jan;11(1):142-157.
2. HRamharter J, et al. J Med Chem. 2021 May 27;64(10):6569-6580.
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