1. Membrane Transporter/Ion Channel
  2. BCRP
  3. BCRP-IN-1

BCRP-IN-1 

Cat. No.: HY-100390 Purity: 98.13% ee.: 98.13%
Handling Instructions

BCRP-IN-1 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.

For research use only. We do not sell to patients.

BCRP-IN-1 Chemical Structure

BCRP-IN-1 Chemical Structure

CAS No. : 1699720-85-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 605 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1750 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Description

BCRP-IN-1 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.

IC50 & 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].

Molecular Weight

355.43

Formula

C₂₀H₂₅N₃O₃

CAS No.

1699720-85-8

SMILES

COC1=CC=C2C(NC3=C2C[[email protected]]4([H])N(C([[email protected]](C)NC4=O)=O)[[email protected]]3CC(C)C)=C1

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (140.67 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8135 mL 14.0675 mL 28.1349 mL
5 mM 0.5627 mL 2.8135 mL 5.6270 mL
10 mM 0.2813 mL 1.4067 mL 2.8135 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.03 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.03 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.03 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Product Name:
BCRP-IN-1
Cat. No.:
HY-100390
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