ML753286

Modify Date: 2024-01-10 12:41:34

ML753286 Structure
ML753286 structure
Common Name ML753286
CAS Number 1699720-89-2 Molecular Weight 355.43
Density N/A Boiling Point N/A
Molecular Formula C20H25N3O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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].

 Names

Name ML753286

 ML753286 Biological Activity

Description 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].
Related Catalog
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 tmax 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]. Animal Model: Male Bcrp KO (Abcg2−/−) and WT (Wistar) Rats[1] 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 tmax 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.
References

[1]. Liao M, et al. Preclinical absorption, distribution, metabolism, excretion and pharmacokinetics of a novelselective inhibitor of breast cancer resistance protein (BCRP). Xenobiotica. 2018 May;48(5):467-477.

 Chemical & Physical Properties

Molecular Formula C20H25N3O3
Molecular Weight 355.43
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