PROTAC BRD4 Degrader-39

Name: PROTAC BRD4 Degrader-39
Brand: TargetMol
SKU: T215155
Rating: 4.5 (1 reviews)

Catalog No. T215155 Copy Product Info

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PROTACBRD4 Degrader-39 is a selective degrader targeting BRD4, with a DC50 value of 24.66 nM. It combines BRDPROTAC(ARV-771) with a carbohydrate, allowing selective delivery to tumor cells with high GLUT1 expression. Upon glutathione activation, ARV-771 is released, leading to BRD4 degradation. This compound can suppress tumor growth without significant toxicity and is useful for cancer research, including studies on breast cancer.

PROTAC BRD4 Degrader-39

Copy Product Info

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Catalog No. T215155

PROTAC BRD4 Degrader-39

Pack Size	Price	USA Stock	Global Stock	Quantity
10 mg	Inquiry	Inquiry	Inquiry
50 mg	Inquiry	Inquiry	Inquiry

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Product Introduction

Bioactivity

Description	PROTACBRD4 Degrader-39 is a selective degrader targeting BRD4, with a DC50 value of 24.66 nM. It combines BRDPROTAC(ARV-771) with a carbohydrate, allowing selective delivery to tumor cells with high GLUT1 expression. Upon glutathione activation, ARV-771 is released, leading to BRD4 degradation. This compound can suppress tumor growth without significant toxicity and is useful for cancer research, including studies on breast cancer.
Targets&IC50	BRD4:24.66 nM (DC50)
In vitro	PROTAC BRD4 Degrader-39 (Compound NG-2) effectively degrades BRD4 in a concentration- and time-dependent manner (0.01-10 μM, 3-48 h) in MDA-MB-231 cells. It relies on glucose transporters and the proteasome for BRD4 degradation. Additionally, PROTAC BRD4 Degrader-39 (5-5000 nM, 3 h) shows efficacy in degrading BRD4 in MDA-MB-157, MCF-7, T-47D, and BEAS-2B cells. Moreover, it is not readily recognized by P-glycoprotein, allowing it to effectively evade efflux in Caco-2 cells.
In vivo	The compound PROTAC BRD4 Degrader-39 (Compound NG-2), administered at a dosage of 2.5 mg/kg via intraperitoneal injection every other day for a total of 14 doses, effectively inhibits tumor growth in the MDA-MB-231 mouse model.

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Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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You can also refer to dose conversion for different animals. More Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc