BI-3406 (compound I-6) 是一种有效的、选择性和口服活性的抑制剂，可抑制 KRAS 和 Son of Sevenless 1 (SOS1) 之间的相互作用，其IC50值为6 nM。BI-3406 可减少 GTP-loaded KRAS 的形成，并抑制MAPK信号通路。BI-3406 具有抗肿瘤的活性。

CAS：2230836-55-0
分子式：C23H25F3N4O3
分子量：462.46
纯度：98%
存储：Store at -20°C

Background:

BI-3406 is an orally active, highly potent and selective between KRAS and Son of Sevenless 1 (SOS1) interaction inhibitor(IC50 of 6 nM),with anticancer activity.

BI-3406 is a interaction between KRAS and its Guanine Nucleotide Exchange Factor (GEF) SOS1 inhibitor. BI-3406 does not block the interaction of KRAS with SOS2 but elicits activity on a broad panel of KRAS oncogenic variants, including all major G12 and G13 oncoproteins. Down-modulation of this signaling cascade by BI-3406 in KRAS G12 or G13 mutant cells effectively limits cell proliferation[2].

参考文献：

1. Michael Gmachl, et al. Novel benzylamino substituted quinazolines and derivatives as sos1 inhibitors. WO2018115380A1.

2. Marco H Hofmann, et al. Abstract PL06-01: Discovery of BI-3406: A potent and selective SOS1::KRAS inhibitor opens a new approach for treating KRAS-driven tumors. December 2019.