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

Cardiovascular Research, Signal Transduction

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