产品说明
生化/生理作用
BAY-293 selectively inhibits SOS1-mediated KRAS activation (IC50 = 52 nM; 50 nM wt or G12C hKRAS & 10 nM SOS1cat) via direct SOS1 binding, blocking SOS1-KRAS interaction (IC50 = 21 nM; 10 nM hSOS1cat & 5 nM hKRAS G12C) without affecting (IC50 >20 μM) CRAF RBD-KRAS interaction, KRAS G12C activation by SOS2, Cdc42 activation by DBS, or EGFR kinase activity. BAY-293 downregulates cellular active RAS (IC50 = 200 nM/Calu-1, 410 nM/HeLa) and downstream ERK phosphorylation (K-562, 150 nM/Calu-1) with good target selectivity as assessed over 358 kinases (<37% inhibition at 1 μM) and a panel of 77 GPCRs, transporters, nuclear receptors and enzymes.
基本信息
经验(实验)分子式 | C25H28N4O2S |
分子量 | 448.58 |
产品性质
质量水平 | 100 |
测定 | ≥98% (HPLC) |
形式 | powder |
旋光性 | [α]/D -85.0 to -103.0°, c = 1.0 in DMSO |
颜色 | white to beige |
溶解性 | DMSO: 2 mg/mL, clear |
储存温度 | −20℃ |
SMILES string | C[C@H](C1=CC(C2=CC=CC=C2CNC)=CS1)NC3=C4C=C(C(OC)=CC4=NC(C)=N3)OC |
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 |