BLU-945

BLU-945 is an inhibitor of mutant EGFR (IC50s = 0. and 0. nM for EGFRL858R/T790M and EGFRL858R/T790M/C797S, respectively). It is selective for these mutants over wild-type EGFR (IC50 = 683 nM) and a panel of greater than 400 kinases at 3 µM. In vivo, BLU-945 (100 mg/kg) induces tumor regression in a mouse xenograft model using H1975 non-small cell lung cancer (NSCLC) cells, which express EGFRL858R/T790M. It inhibits tumor growth in an osimertinib-resistant patient-derived xenograft (PDX) mouse model of NSCLC using tumors harboring EGFRT790M/C797S with an exon 19 deletion.. Solulibility: DMSO: Sparingly soluble: 1-10 mg/ml: Ethanol: Slightly soluble: 0.1-1 mg/ml.