Dasatinib, 10 mg

This small molecule from STEMCELL Technologies is a potent, ATP-competitive tyrosine kinase inhibitor specific for SRC/ABL kinases, including ABL, SRC, LCK, and YES, with IC₅₀ values of < 1.0, 0.5, 0.4, and 0.5 nM, respectively. The compound also demonstrates activity against c-KIT with an IC₅₀ of 5.0 nM and acts as a second-generation inhibitor of the oncogenic tyrosine kinase BCR-ABL, exhibiting 325-fold more potency than Imatinib and the ability to inhibit imatinib-resistant BCR-ABL mutants. In broader screening at 10 µM, the compound inhibits 76 of 148 kinases tested.

Supplied as a crystalline solid, the compound has a chemical formula of C₂₂H₂₆ClN₇O₂S, a molecular weight of 488.0 g/mol, a purity of ≥ 98%, and a CAS number of 302962-49-8. It is also known by the alternative names BMS-354825 and Sprycel.

The product is stable at -20 °C as supplied and remains stable for 12 months from the date of receipt when protected from prolonged exposure to light. The compound is soluble in DMSO at concentrations ≤ 25 mM but has low solubility in aqueous media. Stock solutions should be prepared fresh before use, and final DMSO concentrations above 0.1% should be avoided in cell culture applications due to potential cell toxicity. Published research describes antiproliferative activity in cell lines derived from chronic myeloid leukemia, prostate, breast, and colon tumors, as well as inhibition of imatinib-resistant BCR-ABL mutations.