2248003-60-1

AZD3229 is a potent pan-Kit (c-Kit) mutant inhibitor with GI50 of 1-50 nM in a Kit (c-Kit) mutant-driven Ba/F3 cell line. It also inhibits PDGFR mutants (Tel-PDGFRα, Tel-PDGFRβ, V561D/D842V).

AZD3229 has high bioavailability, low clearance and small volume of distribution in preclinical animal models of mice, rats and dogs. In an in vivo model constructed using the Ba/F3 cell line, AZD3229 at 20 mg/kg bid induces regression of tumor volume more effectively than regorafenib and imatinib at 100 mg/kg qd.

Target	Value
Kit ()
PDGFRα ()
PDGFRβ ()

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