143D is a highly potent and selective, BBB-permeable KRAS G12C inhibitor, inhibits the binding of KRASG12C and SOS1 with IC50 of 21.1 nM.
143D shows little effect on the binding of KRASG12D and SOS1.
143D displays potent antiproliferative activity by causing cell cycle arrest and apoptosis, shows significant antiproliferative effects on the KRASG12C-transformed Ba/F3 cell line with IC50 of 10 nM.
143D selectively inhibits the constitutive activation of KRASG12C signaling pathways.
143D inhibits the KRAS signaling pathway and growth of KRASG12C-mutant tumors.
