ML753286

ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC₅₀ of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species^[1]. IC50 & Target: IC50: 0.6 μM (BCRP)^[1] In Vitro: ML753286 has IC₅₀ values of >30, 0.6, and 39.0 μM for the inhibition of P-gp-, BCRP-, and OATP mediated transport, respectively^[1]. In Vivo: ML753286 (25- or 50-mg/kg (PO); 10 or 20 mg/kg (IV); 0.083-24 hours) appears to completely inhibit Bcrp functions in rats at 25 mg/kg PO or at 20 mg/kg IV. The t_max values in plasma were 1.4, 4.0, and 4.1 hours in Bcrp KO rats, WT rats pre-administered 25-mg/kg ML753286, and WT rats pre-administered 50-mg/kg ML753286, respectively^[1].