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Citarinostat (ACY-241) HDAC inhibitor

Name: Citarinostat (ACY-241)
Brand: Selleck Chemicals
SKU: S8464
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S8464

Citarinostat (ACY-241, HDAC-IN-2) is an orally available selective HDAC6 inhibitor with IC50 of 2.6 nM and 46 nM for HDAC6 and HDAC3, respectively, and has 13 to 18-fold selectivity towards HDAC6 in comparison to HDAC1-3.

Chemical Structure

Molecular Weight: 467.95

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Quality Control

Batch: Purity: 99.82%

99.82

Related Targets	JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Other HDAC Inhibitors	Entinostat (MS-275) RGFP966 Tubastatin A Tubastatin A HCl Fimepinostat (CUDC-907) Trichostatin A (TSA) Mocetinostat (MGCD0103) Ricolinostat (ACY-1215) Quisinostat (JNJ-26481585) Dihydrochloride MC1568

Solubility

In vitro
Batch:

Ethanol : 93 mg/mL

DMSO : 41 mg/mL (87.61 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

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 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.700mg/ml (10.04mM)	Taking the 1 mL working solution as an example, add 50 μL of 94 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.

Chemical Information, Storage & Stability

Molecular Weight	467.95	Formula	C₂₄H₂₆ClN₅O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1316215-12-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	HDAC-IN-2			Smiles	C1=CC=C(C=C1)N(C2=CC=CC=C2Cl)C3=NC=C(C=N3)C(=O)NCCCCCCC(=O)NO

Mechanism of Action

Targets/IC₅₀/Ki	HDAC6 (Cell-free assay) 2.6 nM HDAC1 (Cell-free assay) 35 nM HDAC2 (Cell-free assay) 45 nM HDAC3 (Cell-free assay) 46 nM HDAC8 (Cell-free assay) 137 nM
In vitro	In cell lines from multiple solid tumor lineages, combination treatment with Citarinostat (ACY-241) enhances inhibition of proliferation and increases cell death relative to either single agent alone. This compound also results in more frequent occurrence of mitotic cells with abnormal multipolar spindles and aberrant mitoses, and is associated with increased frequency of abnormal multipolar mitotic spindle formation, induction of aneuploidy, and increased cell death. In A2780 ovarian cancer cells, 24 hour treatment with 300 nM ACY-241 results in increased hyperacetylation of α-tubulin, consistent with inhibition of the tubulin deacetylase HDAC6. Low exposures of it result in selective inhibition of HDAC6, while higher exposures lead to inhibition of Class I HDAC isozymes.
In vivo	Compared to non-selective pan-HDAC inhibitors, Citarinostat (ACY-241) has a favourable safety profile. It has the potential for a substantially reduced side effect profile versus current nonselective HDAC inhibitor drug candidates due to reduced potency against Class I HDACs while retaining the potential for anticancer effectiveness.
References	[1] https://pubmed.ncbi.nlm.nih.gov/27926524/

Applications

Methods	Biomarkers	Images	PMID
Western blot	Ac-Tubulin / Ac-H3K56 Ac-H3K9 Cell viability		27926524

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02935790	Completed	Malignant Melanoma	Celgene\|Syneos Health\|ApoCell Inc.\|Celerion\|NYU Langone Health	September 30 2016	Phase 1
NCT02635061	Terminated	Non Small Cell Lung Cancer	Celgene	August 25 2016	Phase 1
NCT02551185	Completed	Advanced Solid Tumors	Celgene	December 22 2015	Phase 1
NCT02400242	Active not recruiting	Multiple Myeloma	Celgene	May 7 2015	Phase 1

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