Poziotinib

Poziotinib is a potent inhibitor of EGFR family kinases with IC50 values of 3.2, 5.3, 23.5, 4.2, and 2.2 nM for wild-type EGFR, HER2, HER4, EGFRT790M, and EGFRL858R/T790M, respectively. It has greater than 100- to 1,000-fold selectivity for EGFR kinases over 30 other tested kinases in vitro. Poziotinib inhibits growth of wild-type and mutant EGFR kinase-dependent lung, breast, and gastric cancer cell lines (GI50s = 0.6-5.7 nM) and inhibits EGFR phosphorylation and induces apoptosis in vitro. In vivo, poziotinib reduces tumor size in an HCC827 non-small cell lung cancer mouse xenograft model.Formal Name: 1-[4-[[4-[(3,4-dichloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]oxy]-1-piperidinyl]-2-propen-1-one. CAS Number: 1092364-38-9. Synonyms: HM781-36B. Molecular Formula: C23H21Cl2FN4O3. Formula Weight: 491.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 0.3 mg/ml. lambdamax: 231, 251, 331 nm. SMILES: O=C(C=C)N1CCC(OC2=CC(C(NC3=C(F)C(Cl)=C(Cl)C=C3)=NC=N4)=C4C=C2OC)CC1. InChi Code: InChI=1S/C23H21Cl2FN4O3/c1-3-20(31)30-8-6-13(7-9-30)33-19-10-14-17(11-18(19)32-2)27-12-28-23(14)29-16-5-4-15(24)21(25)22(16)26/h3-5,10-13H,1,6-9H2,2H3,(H,27,28,29). InChi Key: LPFWVDIFUFFKJU-UHFFFAOYSA-N.