BI-2852 |
| Catalog No.GC35513 |
BI-2852 es un inhibidor de KRAS para el bolsillo interruptor I/II (bolsillo SI/II) por diseÑo de fÁrmacos basado en la estructura con afinidad nanomolar. El BI-2852 es mecÁnicamente distinto del inhibidor covalente de KRASG12C (se une al bolsillo del interruptor II) y se une diez veces mÁs fuerte al KRASG12DversusKRASwt(740nM frente a 7,5μM). BI-2852 bloquea GEF, GAP y las interacciones efectoras con KRAS, lo que conduce a la inhibiciÓn de la seÑalizaciÓn posterior y un efecto antiproliferativo en las células mutantes de KRAS.
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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