Molibresib besylate (Synonyms: GSK 525762C; I-BET 762 besylate)

Name: Molibresib besylate
Brand: MedChemExpress
SKU: HY-13032B
Rating: 5.0 (19 reviews)

Cat. No.: HY-13032B Purity: 99.64%: FAQs
Data Sheet SDS COA Handling Instructions

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Molibresib besylate (GSK 525762C; I-BET 762 besylate) is a BET bromodomain inhibitor with IC₅₀ of 32.5-42.5 nM.

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

Molibresib besylate Chemical Structure

CAS No. : 1895049-20-3

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 136	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 136	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 106	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 156	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 456	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 1200	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 19 publication(s) in Google Scholar

Other Forms of Molibresib besylate:

Molibresib In-stock

17 Publications Citing Use of MCE Molibresib besylate

: Molibresib besylate purchased from MedChemExpress. Usage Cited in: Nat Med. 2017 Sep;23(9):1055-1062. [Abstract]; Western blot of WCL of C4-2 cells treated with vehicle (DMSO) or different doses of JQ1 or i-BET for 24 h. Actin is used as a loading control.

: Molibresib besylate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Jun 21;7(25):38319-38332. [Abstract]; iBET762 partially disrupts the interaction between full-length ERG and BRD4 (A), and between T1-E4 ERG and BRD4 (B).

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Description

Molibresib besylate (GSK 525762C; I-BET 762 besylate) is a BET bromodomain inhibitor with IC₅₀ of 32.5-42.5 nM.

IC₅₀ & Target

IC50: 32.5-42.5 nM (BET)^[1]

Clinical Trial

Molecular Weight

582.07

Formula

C₂₈H₂₈ClN₅O₅S

CAS No.

1895049-20-3

Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=C(C2=N[C@@H](CC(NCC)=O)C3=NN=C(C)N3C4=CC=C(OC)C=C24)C=C1.O=S(C5=CC=CC=C5)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (42.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7180 mL	8.5900 mL	17.1801 mL
5 mM	0.3436 mL	1.7180 mL	3.4360 mL
10 mM	0.1718 mL	0.8590 mL	1.7180 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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: ≥ 2.67 mg/mL (4.59 mM); Clear solution

This protocol yields a clear solution of ≥ 2.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (26.7 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: ≥ 2.67 mg/mL (4.59 mM); Clear solution

This protocol yields a clear solution of ≥ 2.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (26.7 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.67 mg/mL (4.59 mM); Clear solution

This protocol yields a clear solution of ≥ 2.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (26.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 99.64%

Select Batch:

Data Sheet (279 KB) SDS (252 KB)

COA (257 KB) RP-HPLC (213 KB)

Handling Instructions (2659 KB)

References

[1]. Nicodeme E, et al. Suppression of inflammation by a synthetic histone mimic. Nature. 2010 Dec 23;468(7327):1119-23. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7180 mL	8.5900 mL	17.1801 mL	42.9502 mL
	5 mM	0.3436 mL	1.7180 mL	3.4360 mL	8.5900 mL
	10 mM	0.1718 mL	0.8590 mL	1.7180 mL	4.2950 mL
	15 mM	0.1145 mL	0.5727 mL	1.1453 mL	2.8633 mL
	20 mM	0.0859 mL	0.4295 mL	0.8590 mL	2.1475 mL
	25 mM	0.0687 mL	0.3436 mL	0.6872 mL	1.7180 mL
	30 mM	0.0573 mL	0.2863 mL	0.5727 mL	1.4317 mL
	40 mM	0.0430 mL	0.2148 mL	0.4295 mL	1.0738 mL

Molibresib besylate 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.

Keywords:

Molibresib besylate1895049-20-3GSK 525762CI-BET 762 besylateEpigenetic Reader DomainInhibitorinhibitorinhibit

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Molibresib besylate (Synonyms: GSK 525762C; I-BET 762 besylate)

Customer Review

Other Forms of Molibresib besylate:

Molibresib besylate Related Antibodies

17 Publications Citing Use of MCE Molibresib besylate

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

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Dilution Calculator

Complete Stock Solution Preparation Table

Molibresib besylate Related Classifications

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