XL647

XL647 is a multi-kinase inhibitor (IC50s = 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, FLT4, and EphB4, respectively). It is selective for these kinases over a panel of 10 tyrosine kinases and 55 serine/threonine kinases at 10 µM. XL647 inhibits growth of A431 cells expressing wild-type EGFR and H1975 non-small cell lung cancer (NSCLC) cells expressing both the activating mutant EGFRL858R and the drug resistance-associated mutant EGFRT790M (IC50s = 13 and 920 nM, respectively). In vivo, XL647 (10, 30, and 100 mg/kg) inhibits tumor growth and EGFR phosphorylation in an H1975 mouse xenograft model in a dose-dependent manner.Formal Name: N-(3,4-dichloro-2-fluorophenyl)-6-methoxy-7-[[(3aalpha,5beta,6aalpha)-octahydro-2-methylcyclopenta[c]pyrrol-5-yl]methoxy]-4-quinazolinamine. CAS Number: 781613-23-8. Synonyms: EXEL-7647, Tesevatinib. Molecular Formula: C24H25Cl2FN4O2. Formula Weight: 491.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, Ethanol: 10 mg/ml. lambdamax: 233, 250, 331 nm. SMILES: ClC1=C(Cl)C(F)=C(NC2=NC=NC3=C2C=C(OC)C(OC[C@@H]4C[C@@](CN(C)C5)([H])[C@@]5([H])C4)=C3)C=C1. InChi Code: InChI=1S/C24H25Cl2FN4O2/c1-31-9-14-5-13(6-15(14)10-31)11-33-21-8-19-16(7-20(21)32-2)24(29-12-28-19)30-18-4-3-17(25)22(26)23(18)27/h3-4,7-8,12-15H,5-6,9-11H2,1-2H3,(H,28,29,30)/t13-,14-,15+. InChi Key: HVXKQKFEHMGHSL-QKDCVEJESA-N.