Product Data Sheet

BI-2852

Catalog No. A24527

main product photo
BI-2852 is a KRAS inhibitor designed to target the switch I/II (SI/II) pocket with nanomolar affinity. Unlike covalent KRAS^G12C inhibitors that bind the switch II pocket, BI-2852 exhibits a distinct mechanism of action and binds preferentially to active KRAS^G12D with \~10-fold greater affinity than KRAS^WT (740 nM vs. 7.5 μM). It disrupts interactions between KRAS and GEFs, GAPs, and effectors, thereby inhibiting downstream signaling and exerting antiproliferative effects in KRAS-mutant cells.
Chemical Information
Catalog NumA24527
M. Wt516.59
FormulaC31H28N6O2
Purity>98%
Storageat -20 °C 3 years (powder form); at -20 °C 6 months (Solution base)
CAS No.2375482-51-0
Synonyms
SMILESOC(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
Biological Activity
DescriptionBI-2852 is a KRAS inhibitor designed to target the switch I/II (SI/II) pocket with nanomolar affinity. Unlike covalent KRAS^G12C inhibitors that bind the switch II pocket, BI-2852 exhibits a distinct mechanism of action and binds preferentially to active KRAS^G12D with \~10-fold greater affinity than KRAS^WT (740 nM vs. 7.5 μM). It disrupts interactions between KRAS and GEFs, GAPs, and effectors, thereby inhibiting downstream signaling and exerting antiproliferative effects in KRAS-mutant cells.
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