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
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.