PROTAC BET Degrader-10

Name: PROTAC BET Degrader-10
Brand: MedChemExpress
SKU: HY-112718
Rating: 4.5 (1 reviews)

Cat. No.: HY-112718 Purity: 98.23%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PROTAC BET Degrader-10 is a potent BET protein BRD4 degrader extracted from patent WO2017007612A1, example 37, connected by ligands for Cereblon and BRD4, with a DC₅₀ of 49 nM.

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

PROTAC BET Degrader-10 Chemical Structure

CAS No. : 1957234-97-7

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 370	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 370	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 270	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 430	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 800	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1200	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1800	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

PROTAC BET Degrader-10 is a potent BET protein BRD4 degrader extracted from patent WO2017007612A1, example 37, connected by ligands for Cereblon and BRD4, with a DC₅₀ of 49 nM^[1].

Molecular Weight

783.29

Formula

C₃₉H₃₉ClN₈O₆S

CAS No.

1957234-97-7

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(NCCCCCC(NCC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)=O)C[C@H]4C5=NN=C(C)N5C6=C(C(C)=C(C)S6)C(C7=CC=C(Cl)C=C7)=N4

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 : 100 mg/mL (127.67 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	1.2767 mL	6.3833 mL	12.7667 mL
5 mM	0.2553 mL	1.2767 mL	2.5533 mL
10 mM	0.1277 mL	0.6383 mL	1.2767 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. 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: ≥ 5 mg/mL (6.38 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

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).

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: 98.23%

Select Batch:

Data Sheet (275 KB) SDS (251 KB)

COA (257 KB) LCMS (98 KB)

Handling Instructions (2659 KB)

References

[1]. James Bradner, et al. Methods to induce targeted protein degradation through bifunctional molecules. WO2017007612A1.

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.2767 mL	6.3833 mL	12.7667 mL	31.9167 mL
	5 mM	0.2553 mL	1.2767 mL	2.5533 mL	6.3833 mL
	10 mM	0.1277 mL	0.6383 mL	1.2767 mL	3.1917 mL
	15 mM	0.0851 mL	0.4256 mL	0.8511 mL	2.1278 mL
	20 mM	0.0638 mL	0.3192 mL	0.6383 mL	1.5958 mL
	25 mM	0.0511 mL	0.2553 mL	0.5107 mL	1.2767 mL
	30 mM	0.0426 mL	0.2128 mL	0.4256 mL	1.0639 mL
	40 mM	0.0319 mL	0.1596 mL	0.3192 mL	0.7979 mL
	50 mM	0.0255 mL	0.1277 mL	0.2553 mL	0.6383 mL
	60 mM	0.0213 mL	0.1064 mL	0.2128 mL	0.5319 mL
	80 mM	0.0160 mL	0.0798 mL	0.1596 mL	0.3990 mL
	100 mM	0.0128 mL	0.0638 mL	0.1277 mL	0.3192 mL