Nilotinib monohydrochloride monohydrate
产品说明书
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同义名 : | 盐酸尼罗替尼一水合物 ;AMN107 monohydrochloride monohydrate; Nilotinib (hydrochloride hydrate); AMN-107 hydrochloride monohydrate; Tasigna; Nilotinib hydrochloride monohydrate |
| CAS号 : | 923288-90-8 | |
| 货号 : | A191440 | |
| 分子式 : | C28H25ClF3N7O2 | |
| 纯度 : | 98+% | |
| 分子量 : | 583.99 | |
| MDL号 : | MFCD18251359 | |
| 存储条件： |
Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Nilotinib monohydrochloride monohydrate is a selective Abl inhibitor designed to interact with the ATP-binding site of BCR-ABL with higher affinity than Imatinib, while being more effective (IC50 < 30 nM) and retaining activity against most BCR-ABL point mutants that confer resistance to Imatinib[1]. Nilotinib monohydrochloride monohydrate exhibits significant antitumor efficacy against GIST xenograft cell lines and Imatinib-resistant GIST cell lines. The parent cell lines GK1C and GK3C demonstrate sensitivity to Imatinib, with IC50 values of 4.59±0.97 µM and 11.15±1.48 µM, respectively. The Imatinib-resistant cell lines GK1C-IR and GK3C-IR exhibit resistance to Imatinib, with IC50 values of 11.74±0.17 µM and 41.37±1.07 µM, respectively[2]. | ||
| 作用机制 | Nilotinib was found to bind to the inactive conformation of Abl as observed for imatinib, resulting differential sensitivity of Abl point mutations by Nilotinib. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.71mL 0.34mL 0.17mL |
8.56mL 1.71mL 0.86mL |
17.12mL 3.42mL 1.71mL |
| 参考文献 |
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