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. Targets and eliminates senescent cells. Orally bioavailable.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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.
Citations for Dasatinib
The citations listed below are publications that use Tocris products. Selected citations for Dasatinib include:
4 Citations: Showing 1 - 4
Breast tumor stiffness instructs bone metastasis via maintenance of mechanical conditioning.
Authors: Ghassan Et al.
Cell Rep 2021;35:109293
Melanoma cells adopt features of both mesenchymal and amoeboid migration within confining channels.
Authors: Jeremy S Et al.
Sci Rep 2021;11:17804
Eliminating senescent chondrogenic progenitor cells enhances chondrogenesis under intermittent hydrostatic pressure for the treatment of OA.
Authors: Ran Et al.
Stem Cell Res Ther 2020;11:199
Resolvin E1 is a pro-repair molecule that promotes intestinal epithelial wound healing.
Authors: Asma Et al.
Proc Natl Acad Sci U S A 2020;117:9477-9482
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