DBPR112

DBPR112 is an inhibitor of EGFR and dual-mutant EGFRL858R/T790M (IC50s = 15 and 48 nM, respectively). It is selective for these kinases over 384 other kinases but does inhibit 11 additional kinases, including JAK3, Blk, and bone marrow tyrosine kinase on chromosome X (BMX), at 10,000 nM. DBPR112 reduces the viability of HCC827 and H1975 non-small cell lung cancer (NSCLC) cells with 50% cytotoxicity concentration values (CC50s) of 25 and 620 nM, respectively. It decreases tumor weight without affecting body weight in a HCC827 mouse xenograft model when administered at doses of 20 or 50 mg/kg per day. InChI: InChI=1S/C32H31N5O3/c1-37(2)18-10-17-27(39)35-25-16-9-15-24(19-25)28-29-31(36-26(20-38)22-11-5-3-6-12-22)33-21-34-32(29)40-30(28)23-13-7-4-8-14-23/h3-17,19,21,26,38H,18,20H2,1-2H3,(H,35,39)(H,33,34,36)/b17-10+/t26-/m1/s1 InChIKey: NQAMTZUVRFRJCZ-VMMYIZNOSA-N SMILES: OC[C@H](C1=CC=CC=C1)NC2=C3C(OC(C4=CC=CC=C4)=C3C5=CC(NC(/C=C/CN(C)C)=O)=CC=C5)=NC=N2