Citarinostat (ACY-241)

Catalog No.S8464 Synonyms: HDAC-IN-2

For research use only.

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. It has 13 to 18-fold selectivity towards HDAC6 in comparison to HDAC1-3.

Citarinostat (ACY-241) Chemical Structure

CAS No. 1316215-12-9

Selleck's Citarinostat (ACY-241) has been cited by 5 Publications

Purity & Quality Control

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Biological Activity

Description 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. It has 13 to 18-fold selectivity towards HDAC6 in comparison to HDAC1-3.
Targets
HDAC6 [1]
(Cell-free assay)
HDAC1 [1]
(Cell-free assay)
HDAC2 [1]
(Cell-free assay)
HDAC3 [1]
(Cell-free assay)
HDAC8 [1]
(Cell-free assay)
2.6 nM 35 nM 45 nM 46 nM 137 nM
In vitro

In cell lines from multiple solid tumor lineages, combination treatment with ACY-241 and paclitaxel enhances inhibition of proliferation and increases cell death relative to either single agent alone. Combination treatment with ACY-241 and paclitaxel 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 ACY-241 result in selective inhibition of HDAC6, while higher exposures lead to inhibition of Class I HDAC isozymes[1].

Assay
Methods Test Index PMID
Western blot Ac-Tubulin / Ac-H3K56 ; Ac-H3K9 ; Cell viability 27926524 28264055
In vivo ACY-241 has a favourable safety profile than non-selective pan-HDAC inhibitors. 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[1].

Protocol (from reference)

Cell Research:[1]
  • Cell lines: A2780 ovarian cancer cells
  • Concentrations: 0.1, 0.3, 0.5, 1, 3 μM
  • Incubation Time: 24 h
  • Method: A2780 cells are cultured with vehicle or a range of ACY-241 concentrations for 24 hours prior to immunoblotting.
Animal Research:[1]
  • Animal Models: Female athymic nude mice (Crl:NU(NCr)-Foxn1nu)
  • Dosages: 50 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 467.95
Formula

C24H26ClN5O3

CAS No. 1316215-12-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C=C1)N(C2=CC=CC=C2Cl)C3=NC=C(C=N3)C(=O)NCCCCCCC(=O)NO

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02935790 Completed Drug: ACY-241|Drug: nivolumab|Drug: ipilimumab Malignant Melanoma Celgene|Syneos Health|ApoCell Inc.|Celerion|NYU Langone Health September 30 2016 Phase 1
NCT02635061 Active not recruiting Drug: ACY-241|Drug: Nivolumab Non Small Cell Lung Cancer Celgene August 25 2016 Phase 1
NCT02551185 Completed Drug: ACY-241 Advanced Solid Tumors Celgene December 22 2015 Phase 1
NCT02400242 Active not recruiting Drug: ACY-241|Drug: Pomalidomide|Drug: Dexamethasone Multiple Myeloma Celgene May 7 2015 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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