Neratinib Maleate

SKU: orb1940948

Description

Irreversible ErbB receptor tyrosine kinase inhibitor.(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.

Key Properties

• CAS Number: 915942-22-2
• MW: 673.11
• Purity: >98% (HPLC)
• Formula: C₃₀H₂₉ClN₆O₃·C₄H₄O₄
• Solubility: In Vitro: DMSO : 250 mg/mL (371.41 mM)

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only