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A1874

A1874 is a much improved nutlin-based, BRD4-degrading PROTAC and is able to degrade its target protein by 98% with nanomolar potency.

A1874 Chemical Structure

A1874 Chemical Structure

CAS: 2064292-12-0

Purity & Quality Control

Batch: Purity: 99.6%
99.6

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Biological Activity

Description A1874 is a much improved nutlin-based, BRD4-degrading PROTAC and is able to degrade its target protein by 98% with nanomolar potency.
Targets
BRD4 [1]
In vitro
In vitro

In HCT116 cells, A1874 causes a 97% decrease in viability and in A375 cells, A1874 causes a 98% loss of viability.A1874 reduced viability of Daudi cells by 70% and of MOLM-13 cells by 95%.[1]
Cell Research Cell lines HCT116 cell lines
Concentrations 0-10 μM
Incubation Time 24 h
Method

Treatment of HCT116 cells for 24 hours with increasing concentrations of A1874 induced a dose-dependent knockdown of BRD4 levels, with near-maximum knockdown by 100 nmol/L and a maximum degradation (Dmax) of BRD4 of 98% of the levels in control(0.1% DMSO-treated) cells.
Experimental Result Images Methods Biomarkers Images PMID
Western blot BRD4 / c-Myc / GAPDH / p53 / p21 30385614
Growth inhibition assay Cell viability Cell viability 30385614

Chemical Information & Solubility

Molecular Weight 1173.59 Formula

C58H62Cl3F2N9O7S
CAS No. 2064292-12-0 SDF --
Smiles CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)NCCOCCOCCOCCNC(=O)C4=CC(=C(C=C4)NC(=O)C5C(C(C(N5)CC(C)(C)C)(C#N)C6=C(C=C(C=C6)Cl)F)C7=C(C(=CC=C7)Cl)F)OC)C8=CC=C(C=C8)Cl)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (85.2 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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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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