1. Membrane Transporter/Ion Channel
  2. BCRP
  3. (S)-ML753286

(S)-ML753286 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.

(S)-ML753286 Chemical Structure

(S)-ML753286 Chemical Structure

CAS No. : 1699720-85-8

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 605 In-stock
Solution
10 mM * 1 mL in DMSO USD 605 In-stock
Solid
5 mg USD 550 In-stock
10 mg USD 850 In-stock
25 mg USD 1750 In-stock
50 mg USD 2750 In-stock
100 mg USD 3950 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of (S)-ML753286:

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

(S)-ML753286 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

(S)-ML753286 (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].

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

Molecular Weight

355.43

Formula

C20H25N3O3

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

COC1=CC=C2C(NC3=C2C[C@]4([H])N(C([C@H](C)NC4=O)=O)[C@H]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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (140.67 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.25% ee.: 98.39%

References
Animal Administration
[1]

Mice[1]
To determine pharmacokinetic profile of (S)-ML753286 and Ko143 in vivo, Sprague-Dawley rats are administered 2.0 mg/kg or 20 mg/kg (S)-ML753286 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 (S)-ML753286 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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8135 mL 14.0675 mL 28.1349 mL 70.3373 mL
5 mM 0.5627 mL 2.8135 mL 5.6270 mL 14.0675 mL
10 mM 0.2813 mL 1.4067 mL 2.8135 mL 7.0337 mL
15 mM 0.1876 mL 0.9378 mL 1.8757 mL 4.6892 mL
20 mM 0.1407 mL 0.7034 mL 1.4067 mL 3.5169 mL
25 mM 0.1125 mL 0.5627 mL 1.1254 mL 2.8135 mL
30 mM 0.0938 mL 0.4689 mL 0.9378 mL 2.3446 mL
40 mM 0.0703 mL 0.3517 mL 0.7034 mL 1.7584 mL
50 mM 0.0563 mL 0.2813 mL 0.5627 mL 1.4067 mL
60 mM 0.0469 mL 0.2345 mL 0.4689 mL 1.1723 mL
80 mM 0.0352 mL 0.1758 mL 0.3517 mL 0.8792 mL
100 mM 0.0281 mL 0.1407 mL 0.2813 mL 0.7034 mL
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(S)-ML753286 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
(S)-ML753286
Cat. No.:
HY-100390
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