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BRD4 degrader-6

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Catalog No. T206915Cas No. 3055207-38-7

BRD4 degrader-6 is a dimeric BDR4PROTAC class degrader with a DC50 of less than 0.1 μM. It effectively induces the ubiquitination and degradation of BDR4, exhibiting anticancer properties.

BRD4 degrader-6

BRD4 degrader-6

😃Good
Catalog No. T206915Cas No. 3055207-38-7
BRD4 degrader-6 is a dimeric BDR4PROTAC class degrader with a DC50 of less than 0.1 μM. It effectively induces the ubiquitination and degradation of BDR4, exhibiting anticancer properties.
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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-6 is a dimeric BDR4PROTAC class degrader with a DC50 of less than 0.1 μM. It effectively induces the ubiquitination and degradation of BDR4, exhibiting anticancer properties.
Targets&IC50
BRD4:<0.1 μM(DC50)
In vitro
BRD4 degrader-6 (example 1) is effective in degrading BRD4 in BRD4 HiBiT cells, with a DC₅₀ of less than 0.11 μM, following a pretreatment of 1.5 nM for 2 hours and an additional treatment for 24 hours. The compound relies on the reversibility of its bonds to dissociate into monomers both in vitro and in vivo, allowing cellular entry, subsequent reformation into dimers within the cells, and subsequent binding to the target protein, which leads to ubiquitin-proteasome degradation of the target protein.
Chemical Properties
Molecular Weight1152.67
FormulaC61H71BClN9O7S2
Cas No.3055207-38-7
SmilesC(CNC(C[C@H]1C=2N(C3=C(C(=N1)C4=CC=C(Cl)C=C4)C(C)=C(C)S3)C(C)=NN2)=O)[C@]56[C@](C[C@@]7(C(C)(C)[C@]5(C7)[H])[H])(OB(O6)C8=C(CCC(N[C@H](C(=O)N9[C@H](C(NCC%10=CC=C(C=C%10)C%11=C(C)N=CS%11)=O)C[C@@H](O)C9)C(C)(C)C)=O)C=CC=C8)[H]
Storage & Solubility Information
StoragePowder: -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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
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Dose Conversion

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Tech Support

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
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