PROTAC BET Degrader-1

Name: PROTAC BET Degrader-1
Brand: MedChemExpress
SKU: HY-103633
Rating: 4.5 (1 reviews)

Cat. No.: HY-103633 Purity: 98.15%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.

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

PROTAC BET Degrader-1 Chemical Structure

CAS No. : 2093386-22-0

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 605	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 605	In-stock	Estimated Time of Arrival: December 31
Solid
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 1850	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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

Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE PROTAC BET Degrader-1

•ACS Pharmacol Transl Sci. 2021 Feb 26.

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

Biological Activity
Purity & Documentation
References
Customer Review

Description

PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.

IC₅₀ & Target

BET^[1]

In Vitro

PROTAC BET Degrader-1 (Compound 9) is a potent BET degrader based on PROTAC, decreases the level of BRD2, BRD3, and BRD4 proteins in RS4;11 cells at 3-10 nM, and inhibits the growth of this cell line with an IC₅₀ of 4.3 nM, and 45.5 nM for MOLM-13 cells^[1].

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

Molecular Weight

871.90

Formula

C₄₄H₄₅N₁₁O₉

CAS No.

2093386-22-0

Appearance

Solid

Color

Light yellow to yellow

SMILES

CCN1C(NC2=C3C4=CC(OC)=C(C(C(C)=NO5)=C5C)C=C4NC3=NC(C(NCCCCNC(COC6=C(C(N7C(CCC8=O)C(N8)=O)=O)C(C7=O)=CC=C6)=O)=O)=N2)=CC(C9CC9)=N1

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 (57.35 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	1.1469 mL	5.7346 mL	11.4692 mL
5 mM	0.2294 mL	1.1469 mL	2.2938 mL
10 mM	0.1147 mL	0.5735 mL	1.1469 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)

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: ≥ 1.67 mg/mL (1.92 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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% Corn Oil
Solubility: ≥ 1.67 mg/mL (1.92 mM); Suspended solution

This protocol yields a suspended solution of ≥ 1.67 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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).

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: 98.30%

Select Batch:

Data Sheet (272 KB) SDS (0 KB)

COA (249 KB) HNMR (220 KB) LCMS (135 KB)

Handling Instructions (2659 KB)

References

[1]. Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.1469 mL	5.7346 mL	11.4692 mL	28.6730 mL
	5 mM	0.2294 mL	1.1469 mL	2.2938 mL	5.7346 mL
	10 mM	0.1147 mL	0.5735 mL	1.1469 mL	2.8673 mL
	15 mM	0.0765 mL	0.3823 mL	0.7646 mL	1.9115 mL
	20 mM	0.0573 mL	0.2867 mL	0.5735 mL	1.4337 mL
	25 mM	0.0459 mL	0.2294 mL	0.4588 mL	1.1469 mL
	30 mM	0.0382 mL	0.1912 mL	0.3823 mL	0.9558 mL
	40 mM	0.0287 mL	0.1434 mL	0.2867 mL	0.7168 mL
	50 mM	0.0229 mL	0.1147 mL	0.2294 mL	0.5735 mL