Poziotinib

Poziotinib
  • Name: Poziotinib; HM-781-36; HM-781-36B; NOV-1201;NOV-120101
  • Catalog No.: CPDB0101
  • CAS No.: 1092364-38-9
  • Molecular Weight: 491.3
  • Chemical Formula: C23H21Cl2FN4O3
  • For scientific research only, not for patients.

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    Chemical Name:

    1-(4-((4-((3,4-dichloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)piperidin-1-yl)prop-2-en-1-one

    SMILES Code: 

    C=CC(N1CCC(OC2=CC3=C(NC4=CC=C(Cl)C(Cl)=C4F)N=CN=C3C=C2OC)CC1)=O

    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

    Keyword:

    Poziotinib, HM-781-36, HM-781-36B, NOV-1201,NOV-120101, 1092364-38-9

    Solubility: Soluble in DMSO

    Storage: 0 - 4°C for short term (days to weeks), or -20°C for long term (months)

    Description: 

    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. Formulations containing poziotinib are under investigation in clinical trials for the treatment of EGFR-mutant lung adenocarcinoma.

    Target: EGFR


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