Dasatinib, Free Base (Sprycel, BMS-354825, CAS 302962-49-8, CAS 863127-77-9), >99%

LC Laboratories' Product Number D-3307 - Dasatinib, Free Base (Sprycel, BMS-354825), >99% - for research use only. Small molecule inhibitor of both the SRC and BCR/ABL tyrosine kinases, with IC50's for the isolated kinases of 0.55 and 3.0 nM, respectively. Dasatinib also inhibits Lyn (IC50 = 8.5 nM) and Src (IC50 = 3.0 nM) kinase activities in vitro using 0.1 mg/mL poly (Glu4-Tyr) as the substrate. Dasatinib has greater potency than imatinib mesylate and has activity against the majority of kinase mutations in imatinib-resistant chronic myeloid leukemia. Dasatinib and nilotinib are respectively 325-fold (IC50: 0.6 versus 280 nM) and 20-fold (IC50: 15 versus 280 nM) more potent than imatinib against cells expressing wild-type Bcr-Abl. Similar improvements are also seen in all imatinib-resistant mutants tested, with the exception of T315I. Both inhibitors have activity against imatinib-refractory chronic myelogenous leukemia. Dasatinib is the active ingredient in the drug sold under the trade name Sprycel®. This drug has been approved in at least one country for use in patients with Philadelphia chromosome-positive acute lymphoblastic leukemia and chronic myelogenous leukemia. It is also being tested for use in metastatic melanoma.

• Supplier: LC Laboratories
• Product #: D-3307
• Sku #: D-3307_5g