BI-2852 |
| カタログ番号GC35513 |
BI-2852 は、ナノモルの親和性を持つ構造ベースの薬物設計によるスイッチ I/II ポケット (SI/II ポケット) の KRAS 阻害剤です。 BI-2852 は、共有結合型 KRASG12C 阻害剤と機構的に異なり（スイッチ II ポケットに結合）、活性型 KRASG12D と KRASwt の 10 倍強く結合します（740 nM 対 7.5 μM）。 BI-2852 は、GEF、GAP、および KRAS とのエフェクターの相互作用をブロックし、下流のシグナル伝達の阻害と KRAS 変異細胞の抗増殖効果をもたらします。
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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