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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-BI-3406
BI-3406

Chemical Structure : BI-3406

CAS No.: 2230836-55-0

BI-3406 (BI 3406, BI3406)

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.

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10 mg ¥2180 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 462.473
分子式 C23H25F3N4O3
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

N-[(1R)-1-[3-amino-5-(trifluoromethyl)phenyl]ethyl]-7-methoxy-2-methyl-6-[[(3S)-tetrahydro-3-furanyl]oxy]-4-quinazolinamine

参考文献

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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