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imatinib mesylate

" in TargetMol Product Catalog
  • Inhibitors & Agonists
    3
    TargetMol | Inhibitors_Agonists
Imatinib Mesylate
STI-571, ST-1571 Mesylate, CGP-57148B
T1621220127-57-1
Imatinib Mesylate (STI-571) is a tyrosine kinase receptor inhibitor with antineoplastic activity (IC50s: 0.6 μM, 0.1 μM and 0.1 μM for v-Abl, c-Kit and PDGFR, respectively).
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TargetMol | Inhibitor Hot
N-Desmethyl imatinib mesylate
Norimatinib mesylate, ImatinibmetaboliteN-Desmethylimatinibmesylate
T40504404844-03-7
Norimatinib mesylate, also known as N-Desmethyl imatinib mesylate, is a metabolite derived from Imatinib, which acts as a potent multi-target inhibitor of v-Abl, c-Kit, and PDGFR.
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AP23464
T68581845895-51-4
AP23464 is a potent adenosine 5'-triphosphate (ATP)-based inhibitor of Src and Abl kinases, displays antiproliferative activity against a human CML cell line and Bcr-Abl-transduced Ba F3 cells (IC(50) = 14 nM. AP23464 ablates Bcr-Abl tyrosine phosphorylation, blocks cell cycle progression, and promotes apoptosis of Bcr-Abl-expressing cells. Biochemical assays with purified glutathione S transferase (GST)-Abl kinase domain confirmed that AP23464 directly inhibits Abl activity. Importantly, the low nanomolar cellular and biochemical inhibitory properties of AP23464 extend to frequently observed imatinib mesylate-resistant Bcr-Abl mutants, including nucleotide binding P-loop mutants Q252H, Y253F, E255K, C-terminal loop mutant M351T, and activation loop mutant H396P. AP23464 was ineffective against mutant T315I, an imatinib mesylate contact residue. The potency of AP23464 against imatinib mesylate-refractory Bcr-Abl and its distinct binding mode relative to imatinib mesylate warr......
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6-8 weeks
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