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[BMS-354825] [Sprycel]
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Size |
US $ |
€ |
£ |
¥ |
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100 mg |
263 |
218 |
145 |
31600 |
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300 mg |
515 |
427 |
283 |
61800 |
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1 g |
985 |
818 |
542 |
118200 |
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| US Dollars ($) | European Union Euros (€) | British Pounds (£) | Japanese Yen (¥) |
M.W. 488.02
C22H26ClN7O2S
[302962-49-8]
M.I. 14: 2829
Storage: Store at or below -20 ºC. Solubility: Very soluble in DMSO, up to about 200 mg/mL; very poorly soluble in water or ethanol. Disposal: A
View the MSDS for this product
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 is currently approved 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.
The CAS number for the monohydrate form of dasatinib is [863127-77-9].
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) Section 68B of the Patents Act of 1953 in New Zealand; (vi) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (vii) 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.
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