Dasatinib, 100 mg

From STEMCELL Technologies, this small molecule is a potent, ATP-competitive tyrosine kinase inhibitor that targets SRC/ABL kinases, including ABL, SRC, LCK, and YES with IC₅₀ values of < 1.0, 0.5, 0.4, and 0.5 nM, respectively. It also demonstrates activity against c-KIT with an IC₅₀ of 5.0 nM. As a second-generation inhibitor of the oncogenic tyrosine kinase BCR-ABL, the compound is 325-fold more potent than Imatinib and is able to inhibit imatinib-resistant BCR-ABL mutants. When screened at 10 µM, it inhibited 76 of 148 kinases tested. The product is supplied as a crystalline solid with a purity of ≥ 98%, stable for 12 months from the date of receipt when stored at -20°C. It is soluble in DMSO at ≤ 25 mM but has low solubility in aqueous media, and stock solutions should be diluted into culture medium immediately before use.

In published cancer research applications, the compound inhibits proliferation in cell lines derived from chronic myeloid leukemia (CML), prostate, breast, and colon tumors. It also inhibits proliferation of cells with imatinib-resistant BCR-ABL mutations, inhibits tumor growth and lymph node metastases in orthotopic nude mouse models of prostate cancer, and induces cell-cycle arrest and apoptosis in thyroid cancer cells. Additional studies report that the compound inhibits production of extracellular matrix proteins in dermal fibroblasts and prevents development of bleomycin-challenge-induced fibrosis in mice.