2230836-55-0

BI-3406 (compound I-6) is an orally active, highly potent and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with an IC50 of 6 nM. BI-3406 potently reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 has anticancer activity[1][2].

KRAS-SOS1: 6 nM (IC₅₀)

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[1] Michael Gmachl, et al. Novel benzylamino substituted quinazolines and derivatives as sos1 inhibitors. WO2018115380A1.
[2] Marco H Hofmann, et al. Abstract PL06-01: Discovery of BI-3406: A potent and selective SOS1::KRAS inhibitor opens a new approach for treating KRAS-driven tumors. December 2019.