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D-3307 Dasatinib, Free Base, >99%

[BMS-354825] [Sprycel]

M.W. 488.01

C22H26ClN7O2S

[302962-49-8]

M.I. 14:  2829

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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• 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).

• 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.  NOTE:  The dasatinib sold by LC Laboratories is NOT Sprycel®, and is NOT for human use.

• The CAS number for the monohydrate form of dasatinib is [863127-77-9].

• Sold for laboratory or manufacturing purposes only; not for human, medical, 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.