质量水平
检测方案
≥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°C
SMILES字符串
C[C@H](C1=CC(C2=CC=CC=C2CNC)=CS1)NC3=C4C=C(C(OC)=CC4=NC(C)=N3)OC
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.
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
Roman C Hillig et al.
Proceedings of the National Academy of Sciences of the United States of America, 116(7), 2551-2560 (2019-01-27)
Since the late 1980s, mutations in the RAS genes have been recognized as major oncogenes with a high occurrence rate in human cancers. Such mutations reduce the ability of the small GTPase RAS to hydrolyze GTP, keeping this molecular switch
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