Formulation: A crystalline solid
Formal Name: (2E)-N-[4-[[3-chloro-4-(2-pyridinylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide
Purity: ≥98%
Formula Markup: C30H29ClN6O3
Formula Weight: 557
Shelf life (days): 1460
CAS Number: 698387-09-6
Notes: Neratinib is a dual inhibitor of EGFR and HER2 (IC50s = 92 and 59 nM, respectively).{30796} It is selective for EGFR and HER2 over a panel of 12 kinases (IC50s = >5,000 nM) but does inhibit VEGFR2 and Src (IC50s = 800 and 1,400 nM, respectively). Neratinib inhibits the proliferation of NCI H508 colorectal cancer cells expressing wild-type or mutant forms of HER2 (IC50s = 0.2-3 nM).{30794} It reduces tumor growth in BT474 breast and SKOV3 ovarian cancer mouse xenograft models when administered at a dose of 40 mg/kg.{30796} Formulations containing neratinib have been used in the treatment of breast cancer.
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