BI-2852

产品名称：

2375482-51-0
BI-2852
(S)-5-Hydroxy-3-(2-(((1-((1-methyl-1H-imidazol-4-yl)methyl)-1H-indol-6-yl)methylamino)methyl)-1H-indol-3-yl)isoindolin-1-one
(3S)-2,3-Dihydro-5-hydroxy-3-[2-[[[[1-[(1-methyl-1H-imidazol-4-yl)methyl]-1H-indol-6-yl]methyl]amino]methyl]-1H-indol-3-yl]-1H-isoindol-1-one
BI 2852
BI2852

产品介绍：

产品说明

生化/生理作用

BI-2852 is RAS inhibitor that binds RAS switch I and II (SI/II) pocket in both the active and inactive forms (GCP-/GDP-bound KD in μM = 0.74/2.0 (KRAS-G12D), 7.5/1.1 (KRAS), 0.57/2.5 (HRAS), 1.3/8.3 (NRAS)). BI-2852 inhibits RAS-mediated signaling and proliferation of KRAS-G12C-bearing NCI-H358 lung cancer cells (EGF-induced pERK IC50 = 5.8 μM; GI50 = 6.7 μM in soft agar with low serum) by blocking KRAS interactions with GEF SOS1 (GDP-bound G12C/G12D IC50 = 450/260 nM, GTP-bound Wt/G12C/G12D IC50 = 490/360/490 nM) and effectors CRAF (GTP-bound Wt/G12C/G12D IC50 = 1740/80/770 nM) and PI3Kα (GTP-bound Wt/G12C/G12D IC50 = 250/100/500 nM).

基本信息

经验(实验)分子式	C₃₁H₂₈N₆O₂
分子量	516.59
MDL编号	MFCD32197229

产品性质

质量水平	100
测定	≥98% (HPLC)
形式	powder
颜色	white to beige
溶解性	DMSO: 2 mg/mL, clear
储存温度	2-8℃
SMILES string	O=C1C2=C([C@H](N1)C3=C(NC4=C3C=CC=C4)CNCC5=CC6=C(C=C5)C=CN6CC7=CN(C=N7)C)C=C(C=C2)O

安全信息

储存分类代码	11 - Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable