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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