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BRD4 degrader AT1

Name: BRD4 degrader AT1
Brand: TargetMol
SKU: T5439
Rating: 4.5 (1 reviews)

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Catalog No. T5439Cas No. 2098836-45-2

BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.

BRD4 degrader AT1

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Catalog No. T5439Cas No. 2098836-45-2

BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
5 mg	$1,590	35 days	35 days

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Product Introduction

Bioactivity

Description	BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.
Targets&IC50	BRD2 BD1:111 nM (Kd), BRD3 BD2:39 nM (Kd), BRD4 BD2QVK:38.8 nM (Kd), BRD4 BD2:44 nM (Kd), BRD4 BD1:75 nM (Kd), BRD2 BD2:94 nM (Kd), BRD3 BD1:35 nM (Kd), BRD2 BD1 KEA:35 nM (Kd)
In vitro	BRD4 degrader AT1 is a highly selective Brd4 degrader, exhibiting a Kd of 44 nM for Brd4BD2 in cells, and shows Kds of 38.8 nM for mutant Brd4BD2 (QVK), 111 ± 14 nM for Brd2BD1, 94 ± 9 nM for Brd2BD2, 35 ± 3 nM for Brd3BD1, 39 ± 8 nM for Brd3BD2, 75 ± 23 nM for Brd4BD1, and 35 ± 4 nM for mutant Brd2BD1 (KEA). At concentrations of 1-3 μM, BRD4 degrader AT1 induces significant Brd4-selective depletion while exhibiting minimal activity against Brd2 and Brd3[1].

Chemical Properties

Molecular Weight	972.68
Formula	C₄₈H₅₈ClN₉O₅S₃
Cas No.	2098836-45-2
Smiles	CC1=C(SC2=C1C(=N[C@H](C3=NN=C(N32)C)CC(=O)NCCCCCCSC(C)(C)[C@@H](C(=O)N4C[C@@H](C[C@H]4C(=O)NCC5=CC=C(C=C5)C6=C(N=CS6)C)O)NC(=O)C)C7=CC=C(C=C7)Cl)C
Relative Density.	1.39 g/cm3 (Predicted)

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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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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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