Belinostat

SKU: orb1298864

Description

Belinostat

Research Area

Cell Biology, Epigenetics & Chromatin, Molecular Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 866323-14-0
• MW: 318.35
• Purity: 99.75% (May vary between batches)
• Formula: C₁₅H₁₄N₂O₄S
• SMILES: S(NC1=CC=CC=C1)(=O)(=O)C2=CC(/C=C/C(NO)=O)=CC=C2
• Target: HDAC|||Autophagy
• Solubility: DMSO:245 mg/mL (769.59 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (15.71 mM)

Bioactivity

• Target IC50:
  HDAC:27 nM (Hela cell)|HDAC6:82 nM
• In Vivo:
  Treatment of nude mice bearing human ovarian and colon tumor xenografts with PXD101 (10-40 mg/kg/day i.p.) for 7 days results in a significant, dose-dependent growth delay without obvious signs of toxicity. Growth delay is also observed in xenografts of cisplatin-resistant ovarian tumor cells. A significant increase in acetylation of H4 is detected in blood and tumor tissues 3 hours after treatment. These findings suggest that PXD101 has potential as a novel antitumor agent.
  Read more...
• In Vitro:
  Belinostat is a novel hydroxamate-type inhibitor of histone deacetylase activity that inhibits histone deacetylase activity in HeLa cell extracts with an IC(50) of 27 nM and induces a concentration-dependent (0.2-5 micro M) increase in acetylation of histone H4 in tumor cell lines.Belinostat is cytotoxic in vitro in a number of tumor cell lines with IC(50)s in the range 0.2-3.4 micro M as determined by a clonogenic assay and induces apoptosis.
  Read more...

Storage & Handling

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

Alternative Names

Belinostat, Autophagy, inhibit, Histone deacetylases, Inhibitor, HDAC, PXD-101, PXD 101, PXD101, PX 105684, PX105684, PX-105684

Compound Identifiers

PubChem CID

6918638