store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Nilotinib hydrochloride(AMN-107 HCl) 是一种可口服的 Bcr-Abl 酪氨酸激酶抑制,具有抗肿瘤活性,可用于调节神经炎症和认知障碍,可用于研究慢性骨髓性白血病。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 279 | 现货 | ||
10 mg | ¥ 393 | 现货 | ||
25 mg | ¥ 658 | 现货 | ||
50 mg | ¥ 979 | 现货 | ||
100 mg | ¥ 1,470 | 现货 | ||
500 mg | ¥ 4,150 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 672 | 现货 |
产品描述 | Nilotinib hydrochloride(AMN-107 HCl) is an orally available Bcr-Abl tyrosine kinase inhibitor with antitumor activity for modulation of neuroinflammation and cognitive deficits, and may be used in studies of chronic myelogenous leukemia. |
靶点活性 | BCR-ABL:<30 nM |
体外活性 |
Nilotinib hydrochloride (AMN107 hydrochloride) is a selective Abl inhibitor designed to interact with the ATP binding site of BCR-ABL with higher affinity than imatinib while being more potent than imatinib (IC50<30 nM ), also retains activity against most BCR-ABL point mutants that confer resistance to imatinib.[1] Nilotinib hydrochloride showed significant anti-tumor efficacy against GIST xenograft cell lines and imatinib-resistant GIST cell lines, among which the parental cell lines GK1C and GK3C showed imatinib sensitivity with IC50 of 4.59±0.97 μM and 11.15±1.48 μM, respectively.[2] |
体内活性 |
Nilotinib hydrochloride (AMN107 hydrochloride) (40 mg/kg; oral gavage; daily; for 4 weeks; BALB/cSLc-nu/nu mice with GIST xenograft) demonstrated equivalent or superior antitumor effects in BALB/cSLc-nu/nu mice with GIST xenografts. Nilotinib hydrochloride Inhibited tumor growth by 69.6% in GK1X, 85.3% in GK2X, and 47.5% in GK3X xenograft line.[2] Nilotinib hydrochloride exerts significant healing effects on macroscopic and microscopic pathology scores in a rat model of indomethacin-induced enterocolitis and ensures considerable mucosal healing while reducing PDGFR alpha and beta levels and apoptosis in the colon Rating.[3] |
别名 | AMN-107 HCl |
分子量 | 565.98 |
分子式 | C28H23ClF3N7O |
CAS No. | 923288-95-3 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 90 mg/ml (159.02 mM)
Ethanol: 1 mg/ml (1.77 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 1.7668 mL | 8.8342 mL | 17.6685 mL | 44.1712 mL |
DMSO | 5 mM | 0.3534 mL | 1.7668 mL | 3.5337 mL | 8.8342 mL |
10 mM | 0.1767 mL | 0.8834 mL | 1.7668 mL | 4.4171 mL | |
20 mM | 0.0883 mL | 0.4417 mL | 0.8834 mL | 2.2086 mL | |
50 mM | 0.0353 mL | 0.1767 mL | 0.3534 mL | 0.8834 mL | |
100 mM | 0.0177 mL | 0.0883 mL | 0.1767 mL | 0.4417 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。
Nilotinib hydrochloride 923288-95-3 Angiogenesis Autophagy Cytoskeletal Signaling Tyrosine Kinase/Adaptors Bcr-Abl Nilotinib Hydrochloride AMN-107 HCl Inhibitor inhibitor inhibit