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Domatinostat (4SC-202) HDAC inhibitor

Name: Domatinostat (4SC-202)
Brand: Selleck Chemicals
SKU: S7555
Availability: InStock
Rating: 5 (13 reviews)

Cat.No.S7555

Domatinostat (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. This compound also displays inhibitory activity against Lysine specific demethylase 1 (LSD1) and is in Phase 1.

Chemical Structure

Molecular Weight: 447.51

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.84%

99.84

Related Targets	Epigenetic Reader Domain JAK Histone Methyltransferase AMPK PKC PARP HIF Histone Acetyltransferase Aurora Kinase Sirtuin PRMT Histone Demethylase EZH1/2 DNA Methyltransferase Pim LSD1 MLL JMJD G9a/GLP NSD FTO MicroRNA PAD SETD SMYD DOT1 COMT WDR5 HNMT SAM MTase
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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
CRL-2105	Cell viability assay	72 h	IC50=170 nM	30885250
MyLa	Cell viability assay	72 h	IC50=190 nM	30885250
CRL-8294	Cell viability assay	72 h	IC50=260 nM	30885250
HTB-176	Cell viability assay	72 h	IC50=370 nM	30885250
Se-Ax	Cell viability assay	72 h	IC50=250 nM	30885250
HuT 78	Cell viability assay	72 h	IC50=330 nM	30885250
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	447.51	Formula	C₂₃H₂₁N₅O₃S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	910462-43-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Solubility

In vitro
Batch:

DMSO : 89 mg/mL ( (198.87 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

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.	4.450mg/ml (9.94mM)	Taking the 1 mL working solution as an example, add 50 μL of 89 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.	0.450mg/ml (1.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 9 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.
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.

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	HDAC3 ^[1] (Cell-free assay) 0.57 μM HDAC2 ^[1] (Cell-free assay) 1.12 μM HDAC1 ^[1] (Cell-free assay) 1.20 μM HDAC11 ^[1] (Cell-free assay) 9.7 μM HDAC5 ^[1] (Cell-free assay) 11.3 μM HDAC10 ^[1] (Cell-free assay) 21 μM HDAC9 ^[1] (Cell-free assay) 50 μM
In vitro	In HeLa cells, Domatinostat (4SC-202) induces hyperacetylation of histone H3 with EC50 of 1.1 μM. It induces a G2/M cell cycle arrest by interfering with the normal development of the mitotic spindle and causing collapsed spindle apparatus and multiple nucleation centres. In addition, this compound shows a broad anti-proliferative activity towards human cancer cell lines with a mean IC50 of 0.7 μM. ^[1]
In vivo	Domatinostat (4SC-202) has high oral bioavailability in vivo, and shows high metabolic stability and a low plasma clearance. It (120 mg/kg p.o.) shows pronounced and robust anti-tumor activity in both A549 NSCLC xenograft and RKO27 colon carcinoma model. ^[1]
References	http://www.4sc.de/wp-content/uploads/4SC-202-Poster-EORTC-Berlin-2010.pdf https://pubmed.ncbi.nlm.nih.gov/26831668/

Applications

Methods	Biomarkers	Images	PMID
Western blot	Ac α-tubulin / Ac Histone H3 / Ac Histone H4 Cyclin A / Cyclin B1 / Cyclin D1 / Cyclin E / p21 Caspase-3 / Cleaved Caspase-3 / H3K4me2 / H3K9ac		27250763
Growth inhibition assay	Cell viability IC50		27250763

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01344707	Completed	Advanced Hematologic Malignancies	4SC AG	March 2011	Phase 1

Tech Support

Handling Instructions

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

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

Frequently Asked Questions

Question 1:
Do you have suggestions about the in vivo formulation of it?

Answer:
For in vivo study, we recommend to use 2% DMSO+30% PEG 300+5% Tween 80+ddH2O with solubility up to 10mg/ml for it.

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