EDO-S101

SKU: orb1304127

Description

EDO-S101 (Tinostamustine) is a potent pan-HDAC inhibitor, exhibiting IC50 values of 9, 9, and 25 nM against HDAC1, HDAC2, and HDAC3, respectively. It is utilized in cancer research for its dual alkylating and HDAC inhibitory activity, showing efficacy in both in vitro and in vivo preclinical studies against hematological and solid tumor models.

Research Area

Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 1236199-60-2
• MW: 415.36
• Purity: 98.02%
• Formula: C₁₉H₂₈Cl₂N₄O₂
• SMILES: CN1C=2C(=CC(N(CCCl)CCCl)=CC2)N=C1CCCCCCC(NO)=O
• Target: HDAC
• Solubility: DMSO:30 mg/mL (72.23 mM)

Bioactivity

• Target IC50:
  HDAC2:9nM|HDAC3:25 nM|HDAC1:9nM
• In Vivo:
  Intracellular HDAC inhibition of EDO-S101, which occurs rapidly after dosing is at maximum activity already at the lowest dose of 10 mg/kg and lasts for about 12-16 hours. Exposure to EDO-S101 causes a strong DNA repair response evidenced by activation of pH2AX and p53 in tumors taken from mice bearing subcutaneous human Burkitt's lymphoma. Tumors of BL rapidly shrink or are completely eradicated after i.v. administration of EDO-S101.
• In Vitro:
  EDOS101 inhibits HDAC activity in rat peripheral blood mononuclear cells (PBMCs) in a cellular assay by approximately 90% one hour after dosing with 10 mg/kg i.v. HDAC inhibition in PBMCs could not be increased with higher doses up to 50 mg/kg. EDO-S101 triggers apoptosis and shows strong antitumor activity in HL60 and Daudi cells. Initial in vitro experiments in HL60 cells shows an activation of the intrinsic pathway of apoptosis with cleavage of caspases 3, 9 and PARP and a marked reduction of anti-apoptotic proteins XIAP and Mcl-1.

Storage & Handling

• Storage: store at low temperature,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

Minomustine, inhibit, Inhibitor, EDO-S 101, EDOS101, EDO-S101, EDO-S-101, EDO S101, HDAC8, HDAC6, HDAC, HDAC1, HDAC3, HDAC2, Histone deacetylases, Tinostamustine

Compound Identifiers

PubChem CID

46836227