AZD 9291

AZD 9291 is an inhibitor of mutant EGFRs (IC50s = 1, 12, and 5 nM for EGFRL858R/T790M, EGFRL858R, and EGFRL861Q, respectively). It is selective for these mutant EGFRs over wild-type EGFR (IC50 = 184 nM), as well as over a panel of approximately 280 other kinases at 1 µM. AZD 9291 selectively inhibits the proliferation of mutant EGFR-containing non-small cell lung cancer (NSCLC) cells, including H1975 cells containing the L858R activating and T790M resistance mutations, PC-9 cells containing the activating exon 19 deletion, and vandetanib-resistant PC-9 cells, which contain the exon 19 deletion and T790M mutation (IC50s = 11, 8, and 40 nM, respectively), over wild-type EGFR-containing Calu-3 and NCI H2073 NSCLC cells (IC50s = 650 and 461 nM, respectively). It induces tumor regression in a vandetanib-resistant PC-9 mouse xenograft model when administered at doses ranging from 1 to 10 mg/kg. Formulations containing AZD 9291 have been used in the treatment of EGFR mutant-containing NSCLC.Formal Name: N-[2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide. CAS Number: 1421373-65-0. Synonyms: Osimertinib. Molecular Formula: C28H33N7O2. Formula Weight: 499.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 15 mg/ml, Ethanol: 10 mg/ml. lambdamax: 223, 282, 311 nm. SMILES: CN(CCN(C)C)C1=C(NC(C=C)=O)C=C(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)C(OC)=C1. InChi Code: InChI=1S/C28H33N7O2/c1-7-27(36)30-22-16-23(26(37-6)17-25(22)34(4)15-14-33(2)3)32-28-29-13-12-21(31-28)20-18-35(5)24-11-9-8-10-19(20)24/h7-13,16-18H,1,14-15H2,2-6H3,(H,30,36)(H,29,31,32). InChi Key: DUYJMQONPNNFPI-UHFFFAOYSA-N.