Dasatinib

Biological Activity

Dasatinib is a highly potent pan-Src/Bcr-Abl inhibitor (K_i 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.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. 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.
   J.Med.Chem., 2004;47:6658
2. Repurposing of clinically developed drugs for treatment of Middle East Respiratory Syndrome coronavirus infection.
   Dyall et al.
   Antimicrob.Agents Chemother., 2014;58:4885
3. 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.
   J.Med.Chem., 2006;49:6819

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