molecules of the month


potent and selective SOS1/KRAS inhibitor

related cmpd in Ph. I for KRAS+ cancers

from biochemical HTS and SBDD

Cancer Discovery, Aug. 19, 2020

Boehringer Ingelheim, Vienna, AT

Structure of BI-3406
1 min read

BI-3406 is a compound which binds to SOS1, preventing it from activating the oncoprotein KRAS. While inhibition of WT-KRAS and MEK alone are anticipated to be toxic, the combination of a SOS1 inhibitor with a MEK inhibitor appears to have a broader therapeutic index due to synergy in KRAS-driven tumors. A related undisclosed SOS1 inhibitor, BI 1701963, is in clinical development alone and in combination with a MEK inhibitor.

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