Chemical Name: N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide
Biological ActivityDasatinib is a highly potent pan-Src/Bcr-Abl inhibitor (Ki values are 16 and 30 pM, respectively. Inhibits Bcr-Abl, Src, Lck, Fyn, c-kit and Yes with IC50 values in the subnanomolar range. Inhibits proliferation of tumor cells in vitro and exhibits anticancer acivity in vivo in a mouse chronic myelogenous leukemia (CML) xenograft model. Inhibits replication of SARS-CoV and MERS-CoV in vitro (EC50 values are 2.1and 5.5 μM, respectively). Dasatinib also enhances CD3-targeted lentiviral vector-mediated gene transfer by 3 to 10-fold.
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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.
Lombardo et al.
Repurposing of clinically developed drugs for treatment of Middle East Respiratory Syndrome coronavirus infection.
Dyall et al.
Antimicrob.Agents Chemother., 2014;58:4885
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
Das et al.
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