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A1874 PROTAC chemical

Name: A1874
Brand: Selleck Chemicals
SKU: S8785
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S8785

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

Chemical Structure

Molecular Weight: 1173.59

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: Purity: 99.43%

99.43

Related Targets	Epigenetic Reader Domain HDAC JAK Histone Methyltransferase AMPK PKC PARP HIF Histone Acetyltransferase Aurora Kinase Sirtuin PRMT Histone Demethylase EZH1/2 DNA Methyltransferase Pim LSD1 JMJD G9a/GLP MLL NSD FTO MicroRNA PAD SETD SMYD DOT1 COMT WDR5 HNMT
Related Products	dBET6 ARV-825 dBET1 ACBI1 ARV-771 TD-165 YD23 TL12-186 GMB-475 Luxdegalutamide (ARV-766) ARV-393 Setidegrasib (ASP3082) EGNHS

Chemical Information, Storage & Stability

Molecular Weight	1173.59	Formula	C₅₈H₆₂Cl₃F₂N₉O₇S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2064292-12-0	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (85.2 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (4.26mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.625mg/ml (0.53mM)	Taking the 1 mL working solution as an example, add 50 μL of 12.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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.

Mechanism of Action

Targets/IC₅₀/Ki	BRD4 ^[1]
In vitro	In HCT116 cells, A1874 causes a 97% decrease in viability and in A375 cells, this compound causes a 98% loss of viability. It reduced viability of Daudi cells by 70% and of MOLM-13 cells by 95%.^[1]
References	[1] https://pubmed.ncbi.nlm.nih.gov/30385614/

Applications

Methods	Biomarkers	Images	PMID
Western blot	BRD4 / c-Myc / GAPDH / p53 / p21		30385614
Growth inhibition assay	Cell viability Cell viability		30385614

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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