An inhibitor of EGFRs
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Poziotinib

Item No. 22437

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 0.3 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Product 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.1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cha, M.Y., Lee, K.-O., Kim, M., et al. Antitumor activity of HM781-36B, a highly effective pan-HER inhibitor in erlotinib-resistant NSCLC and other EGFR-dependent cancer models. Int. J. Cancer 130(10), 2445-2454 (2012).