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Description: AZD3229 Tosylate is a novel, potent, pan-KIT mutant inhibitor with low nanomolar growth inhibition against a diverse panel of mutant KIT driven Ba/F3 cell lines (GI50=1-50 nM), with good margin to KDR-driven effects and potential for the Treatment of Gastrointestinal Stromal Tumors. It also inhibits PDGFR mutants (Tel-PDGFRalpha, Tel-PDGFRbeta, V561D/D842V). It also demonstrates excellent cross-species pharmacokinetics, shows strong pharmacodynamic inhibition of target, and is active in several in vivo models of GIST. Selectivity over KDR can be rationalized predominantly by the interaction of water molecules with the protein and ligand in the active site, and its kinome selectivity is similar to the best of the approved GIST agents.
References: J Med Chem. 2018 Oct 11; 61(19):8797-8810
Related CAS#:2248003-60-1 (free base)
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