Catalog No.S8464 Synonyms: HDAC-IN-2
Molecular Weight(MW): 467.95
Citarinostat (ACY-241) 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.
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|Description||Citarinostat (ACY-241) 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.|
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.
|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.|
|In vitro||Ethanol||93 mg/mL (198.73 mM)|
|DMSO||41 mg/mL (87.61 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02886065||Recruiting||Smoldering Multiple Myeloma||Massachusetts General Hospital|Celgene|OncoPep Inc.||November 2016||Phase 1|
|NCT02935790||Completed||Malignant Melanoma||Celgene|INC Research|ApoCell Inc.|Celerion|New York University School of Medicine||September 30 2016||Phase 1|
|NCT02635061||Recruiting||Non Small Cell Lung Cancer||Celgene||August 25 2016||Phase 1|
|NCT02551185||Recruiting||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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