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 Action||Neratinib 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 Formula||C30H29ClN6O3 • C4H4O4|
|Solubility||DMSO with warming; very poorly soluble in ethanol; very poorly soluble in water|
|References||Breslin 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|