AZD3229 is a potent, pan-Kit (c-Kit) mutant inhibitor with potent single digit nM growth inhibition against a diverse panel of mutant Kit (c-Kit) driven Ba/F3 cell lines (GI50=1-50 nM), with good margin to KDR-driven effects. It also inhibits PDGFR mutant
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Product Description
Information
AZD3229 is a potent, pan-Kit (c-Kit) mutantinhibitor with potent single digit nM growth inhibition against a diverse panel of mutant Kit (c-Kit) driven Ba/F3 cell lines (GI50=1-50 nM), with good margin to KDR-driven effects. It also inhibitsPDGFR mutants(Tel-PDGFRα, Tel-PDGFRβ, V561D/D842V).
Targets
Kit ; PDGFRα ; PDGFRβ
In vivo
In preclinical species, bioavailability is high and clearance low across all of mouse, rat, and dog. Volume of distribution is low consistent with the neutral structure. In in vivo models using Ba/F3 cell lines, AZD3229 at a dose of 20 mg/kg b.i.d induces tumor volume regression more effectively than regorafenib at a dose of 100 mg/kg q.d and imatinib.
E2320080