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Neratinib maleate
CAS No. : 915942-22-2
MCE 国际站:Neratinib maleate
产品活性:Neratinib (HKI-272) maleate 是一种具有口服活性的、不可逆的、高选择性的 HER2 和 EGFR 抑制剂,IC50 值分别为 59 nM 和 92 nM。
研究领域:JAK/STAT Signaling | Protein Tyrosine Kinase/RTK
作用靶点:EGFR
In Vitro: Neratinib displays no activity against other serine-threonine kinases such as Akt, cyclin D1/cdk4, cyclin E/cdk2, cyclin B1/cdk1, IKK-2, MK-2, PDK1, c-Raf, and Tpl-2, as well as the tyrosine kinase c-Met.
Neratinib (0.5 ng/mL–5 μg/mL, 2 days) inhibits the proliferation of cell lines that show high levels of HER-2 (3T3/neu, SK-Br-3, and BT474) and is much less active in cell lines that express neither HER-2 nor EGFR (3T3, MDA-MB-435, and SW620) .
Neratinib (0-2 nM, 12-16 h) arrests BT474 cell cycle at G1-S phase.
Neratinib results in the inhibition of MAPK and Akt phosphorylation, down-regulation of cyclin D1 levels, and induction of p27.
In Vivo: Neratinib (HKI-272) (0-80 mg/kg/day; i.g.; 42 days) shows anticancer activities against cancer cells that expresses high levels of HER-2 or EGFR.
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