D-3307 Dasatinib, Free Base, >99%

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO at 200 mg/mL; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility. Disposal: A.

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• More than 830 labs worldwide have purchased Dasatinib from LC Labs (either directly from us or from our many distributors, many of whom resell under their own labels).
• 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. Lombardo, L.J., et al. "Discovery of N-(2-chloro-6-methylphneyl)-2-(6-(4-(2-hydroxyethyl)-piperazin-1-yl)-2-methylpyrimidin-4-ylamino) thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in pre-clinical assays." J. Med. Chem. 47: 6658-6661 (2004).
• 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. Nam, S., et al. "Action of the Src Family Kinase Inhibitor, Dasatinib (BMS-354825), on Human Prostate Cancer Cells." Cancer Res. 65: 9185-9189 (2005).
• Dasatinib has greater potency than imatinib mesylate and has activity against the majority of kinase mutations in imatinib-resistant chronic myeloid leukemia. Copland, M., et al. "Dasatinib (BMS-354825) targets an earlier progenitor population than imatinib in primary CML but does not eliminate the quiescent fraction." Blood 107: 4532-4539 (2006).
• 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. O'Hare, T., et al. "In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants." Cancer Res. 65: 4500-4505 (2005).
• The CAS number for the monohydrate form of dasatinib is [863127-77-9].
• Dasatinib is the active ingredient in the drug product 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.  NOTE: THE DASATINIB SOLD BY LC LABORATORIES FOR RESEARCH IS NOT SPRYCEL®, AND IS NOT FOR HUMAN USE.
• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
• Not available in some countries; not available to some institutions; not available for some uses.