Neratinib maleate

SKU: orb1944868

Description

Neratinib maleate is an irreversible, orally bioavailable inhibitor selectively targeting HER2 (IC50=59 nM) and EGFR (IC50=92 nM). It is widely used in preclinical cancer research, demonstrating antitumor activity in both in vitro assays and in vivo models for breast, prostate, and other solid tumors.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 915942-22-2
• MW: 673.11
• Purity: 99.99% (May vary between batches)
• Formula: C₃₄H₃₃ClN₆O₇
• SMILES: OC(=O)\C=C/C(O)=O.CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4ccccn4)c(Cl)c3)c2cc1NC(=O)\C=C\CN(C)C
• Target: HER,EGFR
• Solubility: DMSO:225 mg/mL (334.27 mM)

Bioactivity

• Target IC50:
  EGFR:92 nM|HER2:59 nM
• In Vivo:
  Neratinib maleate (HKI-272) (10, 20, 40, 60 or 80 mg/kg/day; i.g.; 42 days; Female athymic (nude) mice, tumor xenograft) reduced tumor growth in a dose-dependent manner in 3T3/neu, BT474, SK-OV-3, and A431 xenografts, but was o inactive in xenografts of MX-1 and MCF-7. Inhibited phosphorylation of HER-2 in BT474 xenografts. It shows anticancer activities against cancer cells that express high levels of HER-2 or EGFR.
• In Vitro:
  Neratinib maleate (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 (7 days)) and is much less active in cell lines that express neither HER-2 nor EGFR (3T3, MDA-MB-435, and SW620). Neratinib maleate (0-2 nM; 12-16 h) arrests BT474 cell cycle at the G1-S phase. Neratinib maleate results in the inhibition of MAPK and Akt phosphorylation, down-regulation of cyclin D1 levels, and induction of p27.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Neratinib Maleate, HKI 272 Maleate, HKI272 Maleate, HKI-272 Maleate, HKI-272 maleate, HER2, EGFR

Compound Identifiers

PubChem CID

67307512