2013年10月14日星期一

Imatinib mesylate properties

Imatinib mesylate is a small molecule that inhibits the c-Abl protein-tyrosine kinase, a kinase specifically important for proliferation of chronic myelogenous leukemia (CML). A translocation event between chromosomes 9 and 22 generates the Philadelphia chromosome, which then produces the Bcr-Abl fusion protein with aberrant kinase activity that promotes rapid cell proliferation. Imatinib binds up this crucial kinase, halting CML related growth. Imatinib mesylate has further been displayed to inhibit PDGFR and tyrosine kinases associated with c-Kit.

Name:Imatinib mesylate

Molecular Formula:C29H31N7O.CH4O3S

CAS Registry Number:220127-57-1

Appearance:white crystalline powder .

Molecular Weight:589.7084

Boiling Point:754.9 oC at 760 mmHg

Flash Point:410.3 oC

Solubility:Freely soluble in DMSO and soluble in water

Usage:Imatinib intermediates

a small-molecule inhibitor: Imatinib mesylate (also called Gleevec) is a small-molecule inhibitor of the fusion protein Bcr-Abl, the causal agent in chronic myelogenous leukemia.

As an inhibitor of PDGFR, imatinib mesylate appears to have utility in the treatment of a variety of dermatological diseases. Imatinib has been reported to be an effective treatment for FIP1L1-PDGFRalpha  mast cell disease, hypereosinophilic syndrome, and dermatofibrosarcoma protuberans.

Chemical Properties: Off-White Solid

Uses: A tyrosine kinase inhibitor. Highly specific for BCR-ABL, the enzyme associated with chronic myelogenous leukemia (CML) and certain forms of acute lymphoblastic leukemia (ALL)


Usage: Imatinib Mesylate is orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM, respectively. Imatinib also known as Gleevec, Glivec, CGP-57148B, STI-571 & Imatinib.

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