Dasatinib
Cat. No.:YN440045
产品名称: | Dasatinib |
CAS No.: | 302962-49-8 |
Chemical Name: | N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide |
Synonyms: | 达沙替尼; BMS-354825 |
分子量: | 488.01 |
分子式: | C₂₂H₂₆ClN₇O₂S |
SMILES: | O=C(C1=CN=C(S1)NC2=NC(C)=NC(N3CCN(CC3)CCO)=C2)NC4=C(C=CC=C4Cl)C |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | Dasatinib (BMS-354825) 是一种具有口服活性的,ATP 竞争性的,双重Src/Bcr-Abl抑制剂,具有有效的抗肿瘤活性。对 Src 和 Bcr-Abl 的Ki值分别为 16 pM 和 30 pM。 |
IC50和靶点: | [{name:"Bcr-Abl:1.0 nM (IC50)"},{name: "Src:0.5 nM (IC50)"},{name: "lck:0.4 nM (IC50)"},{name: "yes:0.5 nM (IC50)"},{name: "c-kit:5.0 nM (IC50)"},{name: "PDGFRβ:28 nM (IC50)"},{name: "p38:100 nM (IC50)"},{name: "Her1:180 nM (IC50)"},{name: "Her2:710 nM (IC50)"},{name: "FGFR-1:880 nM (IC50)"},{name: "MEK:1700 nM (IC50)"}] |
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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)
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)
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