產品屬性：
產品名稱 | BI-2852 |
規格 | 5mg、10mg、50mg、100mg |
貨號 | EY-01Y16568 |
Cas No.: 2375482-51-0
別名: N/A
化學名: N/A
分子式: C31H28N6O2
分子量: 516.59
溶解度: DMSO: 55 mg/mL (106.47 mM)
儲存條件: Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產品描述：
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 μM and 6.7 μM in soft agar and low serum conditions in NCI-H358 cells[1].
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