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- Dasatinib D8
Dasatinib D8
An internal standard for the quantification of GC- or LC-MS
此产品仅用于科学研究，我们不为任何个人用途提供产品和服务
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包装价格促销价数量
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500ug￥1187.00950.00- +
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1mg￥2225.001780.00- +
- 货号: ajcx29256
- CAS: 1132093-70-9
- 别名: 达沙替尼D8,BMS-354825-d8
- 分子式: C22H18D8ClN7O2S
- 分子量: 496.05
- 纯度: ＞98%
- 溶解度: DMSO: Soluble,Methanol: Soluble
- 储存: Store at -20°C
- 库存: 现货
Background
Dasatinib-d8 is intended for use as an internal standard for the quantification of dasatinib by GC- or LC-MS. Dasatinib is a potent inhibitor of the non-receptor tyrosine kinases Abl and Src as well as other members of the Src family.1,2 It is effective at sub-nanomolar concentrations, inhibiting Src, Abl, and Lck with IC50 values of 0.05, 0.5, and 0.4 nM, respectively.1,3,4 At nanomolar concentrations, dasatinib also blocks the activity of several other receptor and non-receptor tyrosine kinases, plus drug-resistant mutants.3,4 Because of these activities, dasatinib has potential therapeutic value in diseases characterized by elevated levels of these kinases, including some forms of cancer and fibrotic disease.1,5,6,7
1.Lombardo, L.J., Lee, F.Y., Chen, P., et al.Discovery of N-(2-chloro-6-methyl-phenyl)-2-(6-(4-(2-hydroxyethyl)-piperazin-1-yl)-2-methylpyrimidin-4-ylamino)thiazole-5-carboxamide (BMS-354825),a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assaysJ. Med. Chem.47(27)6658-6661(2004) 2.Das, J., Chen, P., Norris, D., et al.2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (Dasatinib, BMS-354825) as a potent pan-Src kinase inhibitorJ. Med. Chem.49(23)6819-6823(2006) 3.Davis, M.I., Hunt, J.P., Herrgard, S., et al.Comprehensive analysis of kinase inhibitor selectivityNat. Biotechnol.29(11)1046-1051(2011) 4.Carter, T.A., Wodicka, L.M., Shah, N.P., et al.Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinasesProc. Natl. Acad. Sci. USA102(31)11011-11016(2005) 5.El-Amm, J., Freeman, A., Patel, N., et al.Bone-targeted therapies in metastatic castration-resistant prostate cancer: Evolving paradigmsProstate Cancer20131-10(2013) 6.Distler, J.H.W., and Distler, O.Intracellular tyrosine kinases as novel targets for anti-fibrotic therapy in systemic sclerosisRheumatology47(Suppl 5)10-11(2008) 7.McFarland, K.L., and Wetzstein, G.A.Chronic myeloid leukemia therapy: Focus on second-generation tyrosine kinase inhibitorsCancer Control16(2)132-140(2009)
