PROTAC BRD4 Degrader-8

Name: PROTAC BRD4 Degrader-8
Brand: MedChemExpress
SKU: HY-138555
Rating: 4.5 (1 reviews)

Cat. No.: HY-138555 Purity: 98.08%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PROTAC BRD4 Degrader-8 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC₅₀s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells.

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

PROTAC BRD4 Degrader-8 Chemical Structure

Size	Price	Stock	Quantity
1 mg	USD 580	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 1350	In-stock	Estimated Time of Arrival: December 31
10 mg		Get quote
50 mg		Get quote

or Bulk Inquiry

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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

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 1.1 nM (BRD4 BD1), 1.4 nM (BRD4 BD2)^[1]

In Vitro

PROTAC BRD4 Degrader-8 (compound 8; 6 days) inhibits the proliferation of PC3 prostate cancer cells, with an IC₅₀ of 28 nM^[1].
PROTAC BRD4 Degrader-8 (4 h) suppresses MYC gene transcript in MV4-11 AML cells, with an IC₅₀ of 11 nM^[1].
PROTAC BRD4 Degrader-8 (4 h) potently degrades the BRD4 protein in PC3 prostate cancer cells, with an DC₅₀ of 7.5 nM^[1].

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

Molecular Weight

1102.23

Formula

C₅₃H₆₁F₂N₉O₁₁S₂

Appearance

Solid

Color

White to off-white

SMILES

O[C@H](C[C@H]1C(NCC2=CC=C(C=C2)C3=C(N=CS3)C)=O)CN1C([C@@H](NC(COCCOCCOCCNC(C4=CC(N(C5=NC=C(F)C=C5F)CC6=CNC7=C6C8=CN(C)C7=O)=C8C=C4CS(=O)(C)=O)=O)=O)C(C)(C)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 90 mg/mL (81.65 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	0.9073 mL	4.5363 mL	9.0725 mL
5 mM	0.1815 mL	0.9073 mL	1.8145 mL
10 mM	0.0907 mL	0.4536 mL	0.9073 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 (protect from light). 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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 4.5 mg/mL (4.08 mM); Clear solution

This protocol yields a clear solution of ≥ 4.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.0 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% Corn Oil
Solubility: ≥ 4.5 mg/mL (4.08 mM); Clear solution

This protocol yields a clear solution of ≥ 4.5 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 (45.0 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 (protect from light)

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: 98.08%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (251 KB) LCMS (102 KB)

Handling Instructions (2659 KB)

References

[1]. Dragovich PS, et, al. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy. J Med Chem. 2021 Mar 11;64(5):2576-2607. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	0.9073 mL	4.5363 mL	9.0725 mL	22.6813 mL
	5 mM	0.1815 mL	0.9073 mL	1.8145 mL	4.5363 mL
	10 mM	0.0907 mL	0.4536 mL	0.9073 mL	2.2681 mL
	15 mM	0.0605 mL	0.3024 mL	0.6048 mL	1.5121 mL
	20 mM	0.0454 mL	0.2268 mL	0.4536 mL	1.1341 mL
	25 mM	0.0363 mL	0.1815 mL	0.3629 mL	0.9073 mL
	30 mM	0.0302 mL	0.1512 mL	0.3024 mL	0.7560 mL
	40 mM	0.0227 mL	0.1134 mL	0.2268 mL	0.5670 mL
	50 mM	0.0181 mL	0.0907 mL	0.1815 mL	0.4536 mL
	60 mM	0.0151 mL	0.0756 mL	0.1512 mL	0.3780 mL
	80 mM	0.0113 mL	0.0567 mL	0.1134 mL	0.2835 mL