AZ 5104

AZ 5104 is an inhibitor of mutant EGFRs (IC50 = 2 nM for EGFRL858R/T790M and EGFRT790M for both) and an active metabolite of AZD 9291 (Cay-16237). It is selective for these mutant EGFRs over wild-type EGFR (IC50 = 33 nM). AZ 5104 is formed from AZD 9291 by the cytochrome P450 (CYP) isoform CYP3A. It decreases proliferation of H1975 non-small cell lung cancer (NSCLC) cells containing the L858R activating and T790M resistance mutations (GI50 = 24 nM). AZ 5104 (2.5-10 mg/kg per day) reduces tumor growth in an H1975 mouse xenograft model.Formal Name: N-[2-[[2-(dimethylamino)ethyl]methylamino]-5-[[4-(1H-indol-3-yl)-2-pyrimidinyl]amino]-4-methoxyphenyl]-2-propenamide. CAS Number: 1421373-98-9. Molecular Formula: C27H31N7O2. Formula Weight: 485.6. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 277, 313 nm. SMILES: CN(CCN(C)C)C1=C(NC(C=C)=O)C=C(NC2=NC=CC(C3=CNC4=C3C=CC=C4)=N2)C(OC)=C1. InChi Code: InChI=1S/C27H31N7O2/c1-6-26(35)30-22-15-23(25(36-5)16-24(22)34(4)14-13-33(2)3)32-27-28-12-11-21(31-27)19-17-29-20-10-8-7-9-18(19)20/h6-12,15-17,29H,1,13-14H2,2-5H3,(H,30,35)(H,28,31,32). InChi Key: IQNVEOMHJHBNHC-UHFFFAOYSA-N.