Catalog No.: PC-38296Not For Human Use, Lab Use Only.
BI-3406 (BI 3406) is a highly potent and selective SOS1-KRAS interaction inhibitor with IC50 of 5 nM, binds to the catalytic domain of SOS1 with Kd of 9.7 nM.
BI-3406 (BI 3406) is a highly potent and selective SOS1-KRAS interaction inhibitor with IC50 of 5 nM, binds to the catalytic domain of SOS1 with Kd of 9.7 nM.
BI-3406 selectively disrupted the protein-protein interaction between K-RasG12C or K-RasG12D with SOS1 over SOS2, inhibited RAS-GTP levels with an IC50 of 83–231 nM in SOS1/KRAS-dependent NCI-H358 (KRAS G12C) and A549 (KRAS G12S) cell, reduces pERK levels in RAS-mutated cell lines with IC50 of 17-57 nM.
BI-3406 reduces formation of GTP-loaded RAS and limits cellular proliferation of a broad range of KRAS-driven cancers.
BI-3406 attenuates feedback reactivation induced by MEK inhibitors and enhances sensitivity of KRAS-dependent cancers to MEK inhibition.
Combined SOS1 and MEK inhibition represents a novel and effective therapeutic concept to address KRAS-driven tumors.
