Chemical structure of dasatinib.
Western blot analysis of extracts from LNCaP cells, untreated (-) or treated with dasatinib (100 nM, 2 hr; +), using Phospho-Src Family (Tyr416) Antibody #2101 (upper) and Src (36D10) Rabbit mAb #2109 (lower).
Dasatinib is supplied as a lyophilized powder. For a 5 mM stock, reconstitute the 5 mg in 2.05 mL DMSO. Working concentrations and length of treatments vary depending on the desired effect, but it is typically used at 50-500 nM for 2-6 hours. Soluble in DMSO at 200 mg/mL; very poorly soluble in ethanol and water with maximum solubility in water estimated to be about 10 μM.
Store lyophilized or in solution at -20ºC, desiccated. Protect from light. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
Dasatinib is a small molecule inhibitor of both the Src and Bcr-Abl tyrosine kinases, with IC50 values of 0.55 and 3.0 nM for the isolated kinases, respectively (1). Imatinib and dasatinib have similar inhibitory mechanisms, but dasatinib displays greater potency in imatinib-resistant cell lines and greater inhibitory effect on platelet derived growth factor (PDGF) (2,3).
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