Cell Signaling Technology

Product Pathways - MAPK Signaling

Dasatinib #9052

Molecular Formula:
C22H26ClN7O2S
Molecular Weight:
488.01 g/mol
Purity:
>99%

Directions for Use

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.

Western Blotting

Western Blotting

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).

Structure

Structure

Chemical structure of dasatinib.

Background

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).

  1. Lombardo, L.J. et al. (2004) J Med Chem 47, 6658-61.
  2. Copland, M. et al. (2006) Blood 107, 4532-9.
  3. Chen, Z. et al. (2006) Mol Pharmacol 69, 1527-33.

Application References

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For Research Use Only. Not For Use In Diagnostic Procedures.

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