Citarinostat

SKU: orb1303944

Description

ACY-241 (Citarinostat) is a selective, orally bioavailable HDAC inhibitor with antineoplastic potential. It induces histone hyperacetylation and gene expression changes, leading to cell cycle arrest and apoptosis in tumor cells. Research applications include in vitro cytotoxicity studies and in vivo models for multiple myeloma and solid tumors.

Research Area

Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 1316215-12-9
• MW: 467.95
• Purity: 97.94% (May vary between batches)
• Formula: C₂₄H₂₆ClN₅O₃
• SMILES: ONC(=O)CCCCCCNC(=O)c1cnc(nc1)N(c1ccccc1)c1ccccc1Cl
• Target: HDAC
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.27 mM);DMSO:37 mg/mL (79.07 mM)

Bioactivity

• Target IC50:
  HDAC6:2.6 nM|HDAC3:46 nM|HDAC8:137 nM|HDAC1:35 nM|HDAC2:45 nM|HDAC7:7300 nM
• 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:
  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.
• Cell Research:
  A2780 cells are cultured with vehicle or a range of ACY-241 concentrations for 24 hours prior to immunoblotting.(Only for Reference)

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Citarinostat, combination, anti-proliferation, anticancer, ACY241, ACY-241, ACY 241, Histone deacetylases, HDAC3, HDAC6, HDAC2, HDAC1, HDAC, HDAC-IN-2, HDAC8, Inhibitor, inhibit, multiple. myeloma, α-tubulin

Compound Identifiers

PubChem CID

53340426