Dasatinib | CAS:302962-49-8

• 価格
• 構造式
• 製品情報
• 製品詳細
• 文献

価格

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構造式

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製品情報

Dasatinib is a potent inhibitor of the non-receptor tyrosine kinases Abl and Src as well as other members of the Src family. 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. At nanomolar concentrations, dasatinib also blocks the activity of several other receptor and non-receptor tyrosine kinases, plus drug resistant mutants. Because of these activities, dasatinib has potential therapeutic value in diseases that are characterized by elevated levels of these kinases, including some forms of cancer and fibrotic disease.

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製品詳細

name	Dasatinib
Formal Name	N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide
CAS Number	302962-49-8
Synonyms	BMS 354825 Sprycel
Molecular Formula	C22H26ClN7O2S
Formula Weight	488.0
Purity	≥98%
Formulation	A crystalline solid
λmax	323 nm
SMILES	O=C(NC1=C(Cl)C=CC=C1C)C(S2)=CN=C2NC3=NC(C)=NC(N4CCN(CCO)CC4)=C3
InChI Code	InChI=1S/C22H26ClN7O2S/c1-14-4-3-5-16(23)20(14)28-21(32)17-13-24-22(33-17)27-18-12-19(26-15(2)25-18)30-8-6-29(7-9-30)10-11-31/h3-5,12-13,31H,6-11H2,1-2H3,(H,28,32)(H,24,25,26,27)
InChI Key	ZBNZXTGUTAYRHI-UHFFFAOYSA-N
Storage	-20°C
Shipping	Room temperature in continental US; may vary elsewhere
Stability	≥ 2 years

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文献

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 assays. Journal of Medicinal Chemistry 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 inhibitor. Journal of Medicinal Chemistry 49(23), 6819-6823 (2006).

3. Davis, M.I., Hunt, J.P., Herrgard, S., et al. Comprehensive analysis of kinase inhibitor selectivity. Nat.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 kinases. Proceedings of the National Academy of Sciences of the United States of America 102(31), 11011-11016 (2005).

5. El-Amm, J., Freeman, A., Patel, N., et al. Bone-targeted therapies in metastatic castration-resistant prostate cancer: Evolving paradigms. Prostate Cancer 2013, 1-10 (2013).

6. Distler, J.H.W., and Distler, O. Intracellular tyrosine kinases as novel targets for anti-fibrotic therapy in systemic sclerosis. Rheumatology 47, 10-11 (2008).

7. McFarland, K.L., and Wetzstein, G.A. Chronic myeloid leukemia therapy: Focus on second-generation tyrosine kinase inhibitors. Cancer Control 16(2), 132-140 (2009).

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