CAS NO: | 2375482-51-0 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | BI-2852 is aKRASinhibitor for the switch I/II pocket (SI/II-pocket) by structure-based drug design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12Cinhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). 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]. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | BI-2852 (Compound 1) (10 nM-10 μM; 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]. | ||||||||||||||||
分子量 | 516.59 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C31H28N6O2 | ||||||||||||||||
CAS 号 | 2375482-51-0 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : 55 mg/mL(106.47 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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