BI-2852 |
| Catalog No.GC35513 |
BI-2852는 나노몰 친화도를 갖는 구조 기반 약물 설계에 의한 스위치 I/II 포켓(SI/II-포켓)에 대한 KRAS 억제제이다. BI-2852는 공유 KRASG12C 억제제(스위치 II 포켓에 결합)와 기계적으로 구별되며 활성 KRASG12D 대 KRASwt(740nM 대 7.5μM)에 10배 더 강하게 결합합니다. BI-2852는 GEF, GAP 및 KRAS와의 이펙터 상호작용을 차단하여 KRAS 돌연변이 세포에서 다운스트림 신호 전달 및 항증식 효과를 억제합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2375482-51-0
Sample solution is provided at 25 µL, 10mM.
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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].
Reference:
[1]. Kessler D, et al. Drugging an undruggable pocket on KRAS. Proc Natl Acad Sci U S A. 2019 Aug 6; 116(32):15823-15829.
Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)
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