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

Domatinostat (4SC-202) Chemical Structure

CAS No. 910462-43-0

Selleck's Domatinostat (4SC-202) has been cited by 5 Publications

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Biological Activity

Description

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. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). Phase 1.

Targets

HDAC3 ^[1] (Cell-free assay)	HDAC2 ^[1] (Cell-free assay)	HDAC1 ^[1] (Cell-free assay)	HDAC11 ^[1] (Cell-free assay)	HDAC5 ^[1] (Cell-free assay)	Click to View More Targets
0.57 μM	1.12 μM	1.20 μM	9.7 μM	11.3 μM	Click to View More Targets

In vitro

In HeLa cells, 4SC-202 induces hyperacetylation of histone H3 with EC50 of 1.1 μM. 4SC-202 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, 4SC-202 shows a broad anti-proliferative activity towards human cancer cell lines with a mean IC50 of 0.7 μM. ^[1]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

CRL-2105	NUXiOmdXS2WubDD2bYFjcWyrdImgZZN{[Xl?	NVTGWY9RPzMkgJno	M{HafmlEPTB;MUewJI5O	NUH6fpg6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C4PFUzPTBpPkOwPFg2OjVyPD;hQi=>
MyLa	MWDD[YxtKH[rYXLpcIl1gSCjc4PhfS=>	M2DNVlcz6oDLaB?=	MW\JR\|UxRTF7MDDuUS=>	NYHjWJdXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C4PFUzPTBpPkOwPFg2OjVyPD;hQi=>
CRL-8294	MnzMR4VtdCC4aXHibYxqfHliYYPzZZk>	M4jU[\|cz6oDLaB?=	NWjO[mFSUUN3ME2yOlAhdk1?	NGPNfIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEi4OVI2OCd-M{C4PFUzPTB:L3G+
HTB-176	NVLUN3YzS2WubDD2bYFjcWyrdImgZZN{[Xl?	NI\kTVc4OuLCiXi=	NH6xW45KSzVyPUO3NEBvVQ>?	Mo\aQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB6OEWyOVAoRjNyOEi1NlUxRC:jPh?=
Se-Ax	NVfjT\|BNS2WubDD2bYFjcWyrdImgZZN{[Xl?	NW\pdZVoPzMkgJno	NWfYbVB{UUN3ME2yOVAhdk1?	MnPaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB6OEWyOVAoRjNyOEi1NlUxRC:jPh?=
HuT 78	Ml3kR4VtdCC4aXHibYxqfHliYYPzZZk>	M3PJflcz6oDLaB?=	NWfMfpJZUUN3ME2zN\|Ahdk1?	NX\yc2pERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C4PFUzPTBpPkOwPFg2OjVyPD;hQi=>

Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	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 30885250
Growth inhibition assay	Cell viability ; IC50	27250763 30885250

In vivo

In vivo, 4SC-202 has a high oral bioavailability, and shows high metabolic stability and a low plasma clearance. 4SC-202 (120 mg/kg p.o.) shows pronounced and robust anti-tumor activity in both A549 NSCLC xenograft and RKO27 colon carcinoma model. ^[1]

Protocol (from reference)

Cell Research:

^[1]

Cell lines: CRC lines (HT-29, HCT-116, HT-15, and DLD-1)
Concentrations: 0.1, 1, 5, 10 μM
Incubation Time: 72 hours
Method:
CRC cell lines (HT-29, HCT-116, HCT-15, and DLD1), the primary human colon cancer cells, or primary human colon epithelial cells were treated with applied concentrations of 4SC-202, cells were further cultured for indicated time, and cell survival was tested by MTT assay or trypan blue staining assay; cell proliferation was tested by clonogenicity assay. Expression of listed proteins was tested by Western blots.
(Only for Reference)

Animal Research:

^[1]

Animal Models: A549 NSCLC xenograft model and RKO27 colon carcinoma model
Dosages: 120 mg/kg
Administration: p.o.
(Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	89 mg/mL (198.87 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order (Data is from Selleck tests instead of citations): 2% DMSO+30% PEG 300+5% Tween 80+ddH2O For best results, use promptly after mixing. Click to purchase: PEG300 Tween 80	10mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight	447.51
Formula	C₂₃H₂₁N₅O₃S
CAS No.	910462-43-0
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CN1C=C(C=N1)C2=CC=C(C=C2)S(=O)(=O)N3C=CC(=C3)C=CC(=O)NC4=CC=CC=C4N

Download Domatinostat (4SC-202) SDF

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.

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01344707	Completed	Drug: 4SC-202	Advanced Hematologic Malignancies	4SC AG	March 2011	Phase 1

(data from https://clinicaltrials.gov, updated on 2021-09-06)

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.

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Frequently Asked Questions

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

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

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