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Background Information:
Dasatinib is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib binds to and inhibits the growth-promoting activities of these kinases. Apparently because of its less stringent binding affinity for the BCR-ABL kinase, dasatinib has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations. SRC-family protein-tyrosine kinases interact with variety of cell-surface receptors and participate in intracellular signal transduction pathways; tumorigenic forms can occur through altered regulation or expression of the endogenous protein and by way of virally-encoded kinase genes.
Reference:
1. Aleshin A, Finn RS. SRC: a century of science brought to the clinic. Neoplasia. 2010 Aug;12(8):599-607. 2: Ravandi F. Dasatinib, an immunomodulator? Blood. 2010 Aug 5; 116(5):673-4. 3: Duckett DR, Cameron MD. Metabolism considerations for kinase inhibitors in cancer treatment. Expert Opin Drug Metab Toxicol. 2010 Oct ;6(10):1175-93. Review.
APIM050138: DASATINIB
CAS No.: 863127-77-9.
Molecular Formula: C22H26ClN7O2S · H2O.
Molecular Weight: 506.02.
Purity: 99% (HPLC).
QC: HPLC,1HNMR, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO and acidic buffer.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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