马来酸来那替尼 T67385

Product Introduction
Bioactivity


英文名: Neratinib maleate

描述: Neratinib maleate (HKI-272 maleate) 是一种不可逆且具有口服活性和高选择性的 HER2 和 EGFR 抑制剂，IC50 值分别为 59 nM 和 92 nM。Neratinib maleate具有抗肿瘤活性，可用于治疗消化系统疾病、呼吸系统疾病、泌尿生殖系统疾病和皮肤和肌肉骨骼疾病，可用于研究乳腺癌和前列腺癌。

体外活性: 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).[1] Neratinib maleate (0-2 nM; 12-16 h) arrests BT474 cell cycle at the G1-S phase.[1] Neratinib maleate results in the inhibition of MAPK and Akt phosphorylation, down-regulation of cyclin D1 levels, and induction of p27.[1]

体内活性: 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.[1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 225.0 mg/mL (334.3 mM)


关键字: HKI 272 Maleate | Neratinib Maleate | HKI272 Maleate | HKI-272 Maleate

相关产品: Methyl 2,5-dihydroxycinnamate | Coprelotamab | Boehmenan | Multi-target kinase inhibitor 2 | Naluzotan | Chalcone | EGFR-IN-87 | Rilematovir | WZ-3146 | AZ7550 hydrochloride

相关库: Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Tyrosine Kinase Inhibitor Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途