Citarinostat (ACY-241)

Catalog No.S8464 Batch:S846401

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Technical Data

Formula

C24H26ClN5O3
Molecular Weight 467.95 CAS No. 1316215-12-9
Solubility (25°C)* In vitro DMSO 93 mg/mL (198.73 mM)
Ethanol 93 mg/mL (198.73 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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].
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 Assay:[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 Study:[1]
  • Animal Models

    Female athymic nude mice (Crl:NU(NCr)-Foxn1nu)

  • Dosages

    50 mg/kg

  • Administration

    i.p.

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

Overexpression of Human ABCB1 and ABCG2 Reduces the Susceptibility of Cancer Cells to the Histone Deacetylase 6-Specific Inhibitor Citarinostat [ Int J Mol Sci, 2021, 22(5)2592] PubMed: 33807514
Prolactin Drives a Dynamic STAT5A/HDAC6/HMGN2 Cis-Regulatory Landscape Exploitable in ER+ Breast Cancer [ Endocrinology, 2021, 162(5)bqab036] PubMed: 33589921
Preclinical validation of Alpha-Enolase (ENO1) as a novel immunometabolic target in multiple myeloma. [ Oncogene, 2020, 39(13):2786-2796] PubMed: 32024967
Combination of ACY-241 and JQ1 Synergistically Suppresses Metastasis of HNSCC via Regulation of MMP-2 and MMP-9 [ Int J Mol Sci, 2020, 21(18)E6873] PubMed: 32961679
Selective Inhibition of HDAC6 Sensitizes Cutaneous T-cell Lymphoma to PI3K Inhibitors [ Oncol Lett, 2020, 20(1):533-540] PubMed: 32565979

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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