Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 282 | 现货 | ||
50 mg | ¥ 398 | 现货 | ||
100 mg | ¥ 573 | 现货 |
产品描述 | Neratinib maleate (HKI-272 maleate) is an irreversible, orally active and highly selective inhibitor of HER2 and EGFR with IC50 values of 59 nM and 92 nM, respectively.Neratinib maleate has antitumor activity and can be used to treat gastrointestinal, respiratory, genitourinary, and cutaneous and musculoskeletal diseases, and can be used to study breast and prostate cancer. used in the study of breast and prostate cancer. |
靶点活性 | HER2:59 nM, EGFR:92 nM |
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] |
别名 | HKI-272 maleate |
分子量 | 673.11 |
分子式 | C34H33ClN6O7 |
CAS No. | 915942-22-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 225.0 mg/mL (334.3 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.4856 mL | 7.4282 mL | 14.8564 mL | 37.141 mL |
5 mM | 0.2971 mL | 1.4856 mL | 2.9713 mL | 7.4282 mL | |
10 mM | 0.1486 mL | 0.7428 mL | 1.4856 mL | 3.7141 mL | |
20 mM | 0.0743 mL | 0.3714 mL | 0.7428 mL | 1.8571 mL | |
50 mM | 0.0297 mL | 0.1486 mL | 0.2971 mL | 0.7428 mL | |
100 mM | 0.0149 mL | 0.0743 mL | 0.1486 mL | 0.3714 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Neratinib maleate 915942-22-2 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR HER HKI 272 Maleate Neratinib Maleate HKI272 Maleate HKI-272 Maleate HKI-272 maleate Inhibitor inhibitor inhibit