(R) -BI-2852

(R) -BI-2852 is the 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.

Product Specifications

CAS Number

[2375482-49-6]

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

Drug Derivative; Ras

Type

Reference compound

Related Pathways

GPCR/G Protein; MAPK/ERK Pathway; Others

Applications

Neuroscience-Neuromodulation

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/r-bi-2852.html

Purity

97.32

Solubility

DMSO : 55 mg/mL (ultrasonic)

Smiles

OC(C=C1)=CC([C@H](C2=C(CNCC3=CC4=C(C=CN4CC5=CN(C)C=N5)C=C3)NC6=CC=CC=C62)N7)=C1C7=O

Molecular Formula

C31H28N6O2

Molecular Weight

516.59

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501

References & Citations

[1]Dirk Kessler, et al. Drugging all RAS isoforms with one pocket. FUTURE MEDICINAL CHEMISTRY|[2]Kessler D, et al. Drugging an undruggable pocket on KRAS. Proc Natl Acad Sci U S A. 2019 Aug 6; 116 (32) :15823-15829.