BI-2852|KRAS inhibitor|CAS 2375482-51-0

Cas No.:	2375482-51-0
Chemical Name:	(3S)-5-Hydroxy-3-[2-[[[1-[(1-methylimidazol-4-yl)methyl]indol-6-yl]methylamino]methyl]-1H-indol-3-yl]-2,3-dihydroisoindol-1-one
Synonyms:	BI-2852,BI 2852,BI2852
SMILES:	O=C1C2C([H])=C([H])C(=C([H])C=2[C@@]([H])(C2C3=C([H])C([H])=C([H])C([H])=C3N([H])C=2C([H])([H])N([H])C([H])([H])C2C([H])=C([H])C3C([H])=C([H])N(C([H])([H])C4=C([H])N(C([H])([H])[H])C([H])=N4)C=3C=2[H])N1[H])O[H]
Formula:	C₃₁H₂₈N₆O₂
M.Wt:	516.59
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[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.

Description:

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].

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