ML753286

ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC 50 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 In Vitro ML753286 has IC 50 values of >30, 0.6, and 39.0 μM for the inhibition of P-gp-, BCRP-, and OATP mediated transport, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Bcrp KO (Abcg2−/−) and WT (Wistar) Rats Dosage: 25- or 50-mg/kg (PO); 10 or 20 mg/kg (IV) (Pharmacokinetic Study) Administration: PO or IV; 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, and 24 hours Result: 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. Form:Solid IC50& Target:IC50: 0.6 μM (BCRP)

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