BI-2493

Names

[ Name ]:
BI-2493

Biological Activity

[Description]:

BI-2493 is a non-covalent and pan KRAS inhibitor. BI-2493 inhibits the interaction of GDP-bound KRAS with SOS1 in a biochemical assay using recombinant proteins with IC50s < 11nM. BI-2493 can be used in studies about KRAS-driven cancers.

[In Vitro]

BI-2493 inhibits the proliferation with IC50 values < 140 nM in Ba/F3 cell lines made dependent on KRAS by transfection of different mutant KRAS oncogenes (e.g., KRAS G12C, KRAS G12D, KRAS G12V)[1].

[In Vivo]

BI-2493(90 mg/kg; gavage) attenuats tumour growth in mice bearing KRAS G12C, G12D, G12V and A146V mutant models, without causing apparent toxicity to the mice[1].

[References]

1. Kim D, et al. Pan-KRAS inhibitor disables oncogenic signalling and tumour growth. Nature. 2023 Jul;619(7968):160-166.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₄H₂₇N₇OS

[ Molecular Weight ]:
461.58

Related Compounds

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