Dasatinib (863127-77-9)

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Product Detail

Mechanism:

Dasatinib is an orally bioavailable synthetic small molecule inhibitor of the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Dasatinib binds to and inhibits the growth-promoting activities of these kinases. Based on modeling studies, Dasatinib is predicted to bind to multiple conformations of the ABL kinase. In vitro, Dasatinib was active in leukemic cell lines representing variants of imatinib mesylate sensitive and resistant disease. 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. Dasatinib inhibited the growth of CML and acute lymphoblastic leukemia (ALL) cell lines over-expressing BCR-ABL. Under the conditions of the assays, Dasatinib was able to overcome imatinib resistance resulting from BCR-ABL kinase domain mutations, activation of alternate signaling pathways involving the SRC family kinases (LYN, HCK), and multi-drug resistance gene overexpression.

Storage conditions: Preserve in tight containers, at room temperature.

Packaging: Polyethylene nylon plastic bag

CAS Number: 863127-77-9

Formula: C22H28ClN7O3S.

Molecular Weight: 506.02082 g/mol

Method of Analysis:In house Monograph

Application:

Dasatinib is a pyrimidine and thiazole derived antineoplastic agent. It is an oral dual BCR/ABL and Src family tyrosine kinase inhibitor approved for use in patients with chronic myelogenous leukemia (CML) ) who are resistant or intolerant to imatinib. It is also indicated for the treatment of adults with Philadelphia chromosome-positive acute lymphoblastic leukemia (ALL) with resistance or intolerance to prior therapy.