BI-2493 is a structural analogue of BI-2865 for in vivo administration, BI-2493 a potent, inactive state selective, non-covalent pan KRAS inhibitor.
BI-2493 is highly selective for KRAS and does not cause more than 30% inhibition in a panel of 404 kinases or 38 targets commonly used in safety profiling .
BI-2493 attenuates tumour growth in mice bearing KRAS G12C, G12D, G12V and A146V mutant models, without causing apparent toxicity to the mice, shows inhibition of ERK phosphorylation and DUSP6 messenger RNA expression in tumour models.
