DZD9008

DZD9008 is an irreversible inhibitor of EGFR containing a lysine-to-arginine mutation at position 858 and T790M (EGFRL858R,T790M, IC50 = 1.1 nM). It is selective for EGFRL858R,T790M over Bruton's tyrosine kinase (BTK), wild-type EGFR, focal adhesion kinase (FAK), HER2, and HER4 (IC50s = 213, 226, 255, 392, and 704 nM, respectively) but also inhibits wild-type EGFR containing an exon 19 deletion, EGFRT790M containing an exon 19 deletion, EGFRL585R, EGFRG192A, and EGFRL861Q (IC50s = 1.3-12 nM). DZD9008 (25 and 50 mg/kg twice per day) reduces tumor volume in a patient-derived xenograft (PDX) mouse model of non-small cell lung cancer (NSCLC).Formal Name: N-[5-[[4-[[5-chloro-4-fluoro-2-(1-hydroxy-1-methylethyl)phenyl]amino]-2-pyrimidinyl]amino]-2-[(3S)-3-(dimethylamino)-1-pyrrolidinyl]-4-methoxyphenyl]-2-propenamide. CAS Number: 2370013-49-1. Molecular Formula: C29H35ClFN7O3. Formula Weight: 584.1. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Soluble. SMILES: CC(C)(O)C(C=C(C(Cl)=C1)F)=C1NC2=NC(NC3=CC(NC(C=C)=O)=C(N4CC[C@H](N(C)C)C4)C=C3OC)=NC=C2. InChi Code: InChI=1S/C29H35ClFN7O3/c1-7-27(39)34-22-14-23(25(41-6)15-24(22)38-11-9-17(16-38)37(4)5)35-28-32-10-8-26(36-28)33-21-13-19(30)20(31)12-18(21)29(2,3)40/h7-8,10,12-15,17,40H,1,9,11,16H2,2-6H3,(H,34,39)(H2,32,33,35,36)/t17-/m0/s1. InChi Key: BTMKEDDEMKKSEF-KRWDZBQOSA-N.