Entinostat

SKU: orb1300954

Description

Entinostat (MS-275) is an orally active, class I-selective HDAC inhibitor targeting HDAC1, HDAC2, and HDAC3. It exhibits potent antitumor activity and is widely used in cancer research, demonstrating efficacy in both in vitro cellular assays and in vivo animal models of various malignancies.

Research Area

Cell Biology, Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 209783-80-2
• MW: 376.41
• Purity: 99.74% (May vary between batches)
• Formula: C₂₁H₂₀N₄O₃
• SMILES: Nc1ccccc1NC(=O)c1ccc(CNC(=O)OCc2cccnc2)cc1
• Target: Autophagy,HDAC,Apoptosis
• Solubility: DMSO:237.5 mg/mL (630.96 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.77 mg/mL (10.02 mM)

Bioactivity

• Target IC50:
  WSU-HN6:0.54 μM|HDAC2:453 nM|HDAC1:0.18 μM(cell free)|HDAC3:0.74 μM(cell free)|WSU-HN12 cells:23.31 μM
• In Vivo:
  METHODS: To assay antitumor activity in vivo, Entinostat (12.5-49 mg/kg, 0.05 N HCl+0.1% Tween 80) was administered orally to nude mice bearing human tumor xenografts five times per week for four weeks. RESULTS: Entinostat at 49 mg/kg showed significant antitumor effects against KB-3-1, 4-1St, and St-4 tumor lines, and moderate effects against Capan-1 tumors. 24.5 mg/kg and 12.3 mg/kg also showed significant effects against these tumors. The dose of 24.5 mg/kg was also effective against A2780 and HT-29 and moderately effective against Calu-3.
• In Vitro:
  METHODS: A variety of tumor cells were treated with Entinostat for 72 h, and cell viability was measured by Resazurin solution. RESULTS: Entinostat inhibited tumor cell proliferation with an average IC50 of 2.57 µM. METHODS: Human pancreatic cancer cells PANC-1 and SUIT2 Clone 1 were treated with Entinostat (1-50 µM) for 72 h. The expression levels of target proteins were measured by Western Blot. RESULTS: Entinostat caused a dose-dependent increase in cellular histone H3 acetylation and had no effect on total histone H3 protein levels, confirming that Entinostat inhibits the deacetylation activity of HDAC in cancer cell lines.
• Cell Research:
  Cancer cells (5 × 10^3) were seeded into each well of 96-well plates and were cultured with graded concentrations of the drugs for 3 days. The cells were stained with 0.1 mg/ml neutral red for 1 h in a CO2-incubator, and, after aspiration of the medium, OD540 of the neutral red solubilized with 50 μl of ethanol and 150 μl of 0.1 M Na2HPO4 was measured. The IC50 value was determined by plotting growth inhibition of the cells against the logarithm of the drug concentration .
• Animal Research:
  A2780 cells (9 × 10^6) grown in vitro were suspended in PBS and were injected subcutaneously into the flank of nude mouse. For the other tumor lines, KB-3-1, HCT-15, 4-1St, Calu-3, St-4, Capan-1, and HT-29, tumors were passaged several times before starting in vivo antitumor testing, and a tumor lump (2–3 mm in diameter) was transplanted subcutaneously into the flank of a nude mouse by using a trocar needle. Treatment (four or five mice in each experimental group) with the drugs was started after the tumors were confirmed to have grown in the body (tumor size, 20–100 mm3). MS-27-275 and compound 2, both dissolved with 0.05 N HCl, 0.1% Tween 80, and 5-fluorouracil (5-FU) and diluted with physiological saline, were administered orally once daily 5 days per week for 4 weeks. Tumor length and width were monitored twice weekly, and tumor volume was calculated as described .

Storage & Handling

• Storage: store at low temperature,keep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Autophagy, Apoptosis, Entinostat, Histone deacetylases, Inhibitor, HDAC3, HDAC, HDAC1, inhibit, MS275, MS-275, MS 275, SNDX 275, SNDX275, SNDX-275

Compound Identifiers

PubChem CID

4261