1699720-85-8

1699720-85-8 structure

Name: (S)-ML753286
Chemical Name: BCRP-IN-1
CAS Number: 1699720-85-8
Molecular Formula: C₂₀H₂₅N₃O₃
Molecular Weight: 355.43
Catalog: Signaling Pathways Membrane Transporter/Ion Channel BCRP
Create Date: 2018-09-30 09:36:51
Modify Date: 2024-01-10 08:04:00
BCRP-IN-1 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.

Name	BCRP-IN-1

Description	BCRP-IN-1 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> BCRP Research Areas >> Cancer
Target	IC50: 0.6 μM (BCRP efflux transporter)[1]
In Vivo	BCRP-IN-1 (Compound A) shows the potency and a potent pharmacokinetic (PK) profile in rats (lower clearance [1.54 L/h/kg] and higher bioavailability [123%]). XL388 has moderate terminal elimination half-life with t1/2s of 0.9 h and 2.0 h for 2 mg/kg (iv) and 20 mg/kg (po) in rats, respectively[1].
Animal Admin	Mice[1] To determine pharmacokinetic profile of BCRP-IN-1 and Ko143 in vivo, Sprague-Dawley rats are administered 2.0 mg/kg or 20 mg/kg BCRP-IN-1 or 2.0 mg/kg or 50 mg/kg Ko143, formulated in 0.5% HPMC/0.2% Tween80, via iv or po, respectively. After administration of BCRP-IN-1 or Ko143, blood is obtained from all animals at predose and at 0.083, 0.25, 0.5, 1, 4, 8, and 24 h postdose. Approximately 200 μL of whole blood is collected from the jugular vein catheter of each animal into tubes containing the anticoagulant dipotassium ethylenediaminetetraacetic acid (K2EDTA) and is further processed into plasma at approximately 4°C[1].
References	[1]. Li Y, et al. Synthesis of a new inhibitor of breast cancer resistance protein with significantly improved pharmacokinetic profiles. Bioorg Med Chem Lett. 2016 Jan 15;26(2):551-555.