BI-2852

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BI-2852

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2375482-51-0

包装与价格：

包装	价格(元)
5mg	询价
10mg	询价
50mg	询价
100mg	询价

BI-2852 是基于药物结构设计的 switch SI/II 口袋的 KRAS 抑制剂，其通过基于结构的药物设计具有纳摩尔亲和力。BI-2852 在机理上不同于共价 KRASG12C 抑制剂 (结合 switch II)，它结合存在于 KRAS 的活性和非活性形式中的不同口袋。BI-2852 阻断 GEF，GAP 和效应子与 KRAS 的相互作用，导致下游信号传导的抑制和 KRAS 突变细胞中的抗增殖作用。

Cas No.	2375482-51-0
Canonical SMILES	OC(C=C1)=CC([C@@H](C2=C(CNCC3=CC4=C(C=CN4CC5=CN(C)C=N5)C=C3)NC6=CC=CC=C62)N7)=C1C7=O
分子式	C₃₁H₂₈N₆O₂
分子量	516.59
溶解度	DMSO: 55 mg/mL (106.47 mM)
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based drug design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) because it binds to a different pocket present in both the active and inactive forms of KRAS. BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells[1]. KRAS(G12C)\|450 nM (IC50)\|KRAS(G12C)\|750 nM (Kd) BI-2852 (Compound 1) (10 nM-10 μ 2 hours) shows a dose-dependent pERK modulation and antiproliferative effect at EC50s of 5.8 &#181M and 6.7 &#181M in soft agar and low serum conditions in NCI-H358 cells[1]. Reference: [1]. Kessler D, et al. Drugging an undruggable pocket on KRAS. Proc Natl Acad Sci U S A. 2019 Aug 6; 116(32):15823-15829.