Nilotinib monohydrochloride monohydrate

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Chemical Structure| 923288-90-8 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 : 583.992
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
溶解度 :

DMSO: 35 mg/mL(59.93 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
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].
实验方案
1mg 5mg 10mg

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

[1]Weisberg E, et al. Beneficial effects of combining nilotinib and imatinib in preclinical models of BCR-ABL+ leukemias. Blood. 2007 Mar 1;109(5):2112-20.

[2]Sako H, et al. Antitumor effect of the tyrosine kinase inhibitor Nilotinib on gastrointestinal stromal tumor (GIST) and Imatinib-resistant GIST cells. PLoS One. 2014 Sep 15;9(9):e107613.

[3]Dervis Hakim G, et al. Mucosal healing effect of nilotinib in indomethacin-induced enterocolitis: A rat model. World J Gastroenterol. 2015 Nov 28;21(44):12576-85.