产品描述:
Ripretinib is an inhibitor of KIT and PDGFRα (IC50s = 3 and 3.6 nM, respectively).{53053} It is selective for KIT and PDGFRα over a panel of 300 kinases (IC50s = >100 nM) but does inhibit DDR2, VEGFR2, PDGFRβ, and Tie2 (IC50s = V654A, KITT670I, KITD816H, KITD816V, and PDGFRαD842V (IC50s = 11, 9.2, 18, 25, and 36 nM, respectively). Ripretinib induces apoptosis in ROSA wild-type, and KITD816V- or KITK509I-expressing mast cells in a concentration-dependent manner.{53054} It reduces tumor growth and increases survival in an imatinib-resistant patient-derived xenograft (PDX) mouse model of gastrointestinal stromal tumors (GISTs) when administered at doses of 50 and 100 mg/kg.{53053} Formulations containing ripretinib have been used in the treatment of GISTs.