(R)-BI-2852( —— )

Catalog No. M36442 CAS No. 2375482-49-6

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

(R)-BI-2852
Note

Research use only, not for human use.
Brief Description

(R)-BI-2852 can be used as (R)-5-isoindolin-1-one is used as an inhibitor of the RAS family of proteins and as a compound for the treatment and prevention of tumours. (R)-BI-2852 has Antiproliferative and antitumour agent activity.
Description

(R)-BI-2852 is the inactive isomer of BI-2852 (HY-126247), and can be used as an experimental control. BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (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.
In Vitro

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In Vivo

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Synonyms

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Pathway

MAPK/ERK Signaling
Target

Ras
Recptor

Ras
Research Area

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Indication

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CAS Number

2375482-49-6
Formula Weight

516.59
Molecular Formula

C31H28N6O2
Purity

>98% (HPLC)
Solubility

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SMILES

C(NCC=1C=C2N(CC3=CN(C)C=N3)C=CC2=CC1)C4=C(C=5C(N4)=CC=CC5)[C@H]6C=7C(C(=O)N6)=CC=C(O)C7
Chemical Name

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1. Dirk Kessler, et al. Drugging all RAS isoforms with one pocket. FUTURE MEDICINAL CHEMISTRY

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