SKU: N068  / 
    CAS Number: 915942-22-2

    Neratinib Maleate

    $146.00 - $221.71
    Neratinib Maleate is the maleate salt form of Neratinib.  Neratinib is a quinoline derivative. It acts as a tyrosine kinase inhibitor and has anticancer properties.  Neratinib has shown benefit for HER2 positive breast cancer and non-small cell lung cancer.
    Mechanism of ActionNeratinib is a dual inhibitor of human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases with similar potency, and the inhibition is irreversible. It targets a cystine residue in the ATP binding pocket of the receptor. It can induce cell cycle arrest and decrease cell proliferation. The inhibition is irreversible.
    Molecular FormulaC30H29ClN6O3 • C4H4O4
    SolubilityDMSO with warming; very poorly soluble in ethanol; very poorly soluble in water
    ReferencesBreslin S and O'Driscoll L (2016) The relevance of using 3D cell cultures, in addition to 2D monolayer cultures, when evaluating breast cancer drug sensitivity and resistance. Oncotarget 7(29):45745-45756 PMID 27304190 Rabindran SK (2004) Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Res. 64(11):3958–3965 PMID 15173008 Zhao X et al (2019) Neratinib (HKI-272) reverses ABCB1-mediated chemotherapeutic drug resistance in vitro, in vivo and ex vivo. Molec. Pharmacol. 95(3) mol.111.076299