Name: dBET57
Brand: Selleck Chemicals
SKU: S0137
Rating: 5 (1 reviews)

dBET57 is a novel, potent and selective degrader of BRD4_BD1 based on the PROTAC technology with DC_50/5h of 500 nM. dBET57 is inactive on BRD4_BD2.

dBET57 Chemical Structure

CAS: 1883863-52-2

Selleck's dBET57 has been cited by 1 publication

Purity & Quality Control

Batch: S013701 DMSO] 100 mg/mL] false] Ethanol] 12 mg/mL] false] Water] Insoluble] false Purity: 99.72%

99.72

dBET57 Related Products

Related Targets	BET p300/CBP BRPF bromodomain	Click to Expand
Related Compound Libraries	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Bioactive Compound Library-Ⅱ	Click to Expand

Signaling Pathway

Epigenetic Reader Domain Signaling Pathway

Choose Selective Epigenetic Reader Domain Inhibitors

Biological Activity

Description

dBET57 is a novel, potent and selective degrader of BRD4_BD1 based on the PROTAC technology with DC_50/5h of 500 nM. dBET57 is inactive on BRD4_BD2.

Targets

BRD4_BD1 ^[1]
(Cell-free assay)

500 nM(DC50)

References

[1] Radosław P Nowak, et al. Nat Chem Biol. 2018 Jul;14(7):706-714.

Chemical Information & Solubility

Molecular Weight	699.18	Formula	C₃₄H₃₁ClN₈O₅S
CAS No.	1883863-52-2	SDF	--
Smiles	CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)NCCNC4=CC=CC5=C4C(=O)N(C5=O)C6CCC(=O)NC6=O)C7=CC=C(C=C7)Cl)C
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (143.02 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 12 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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