Dasatinib is an orally-available, aminothiazole-based inhibitor of Abl and Src at IC50 values of 0.6 and 8 nm, respectively. [1] Dasatinib has been shown to be >300-fold more potent than imatinib in cells expressing wild-type Bcr-Abl and in a number of imatinib-resistant mutants at IC50s < 1.7 nM. [2] With the exception of T315I, Dasatinib inhibited cell proliferation of mutants in the range of 0.8 to 11 nM.
Dasatinib's activity against Lck allows for inhibition of T-cell receptor-mediated signal transduction, cellular proflieration, cytokine production, and in vivo T-cell responses. Combination of dasatinib with other immunomodulators such as cyclosporine A or rapamycin results in a synergistic inhibition of T-cell activation. [3]
Technical information:
| Chemical Formula: | C22H26ClN7O2S | |
| CAS #: | 302962-49-8, 863127-77-9 | |
| Molecular Weight: | 488.01 | |
| Purity: | > 99% | |
| Appearance: | White Crystalline | |
| Chemical Name: | N-(2-chloro-6-methylphenyl)-2-(6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-ylamino)thiazole-5-carboxamide | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | BMS-354825, BMS 354825, BMS354825, Sprycel, dasatinibum, Dasatinib |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | O'Hare et al., In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants. Cancer Res. 2005, 65, 4500-4505. Pubmed ID: 15930265 |
| 2. | Steinberg et al., Dasatinib: a tyrosine kinase inhibitor for the treatment of chronic myelogenous leukemia and philadelphia chromosome-positive acute lymphoblastic leukemia. Clin. Ther. 2007, 29(11), 2289-2308. Pubmed ID: 18158072 |
| 3. | Schade et al., Dasatinib, a small-molecule protein tyrosine kinase inhibitor, inhibits T-cell activation and proliferation. Blood, 2008, 111, 1366-1377. Pubmed ID: 17962511 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
