1. Cell Cycle/DNA Damage
    Epigenetics
  2. HDAC

EDO-S101 (Synonyms: Tinostamustine)

Cat. No.: HY-101780 Purity: 98.09%
Data Sheet SDS Handling Instructions

EDO-S101 is a pan HDAC inhibitor; inhibits HDAC1, HDAC2 and HDAC3 with IC50 values of 9, 9 and 25 nM, respectively.

For research use only. We do not sell to patients.
EDO-S101 Chemical Structure

EDO-S101 Chemical Structure

CAS No. : 1236199-60-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO $320 In-stock
1 mg $110 In-stock
5 mg $350 In-stock
10 mg $600 In-stock
25 mg $1200 In-stock
50 mg $1950 In-stock
100 mg $2800 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

EDO-S101 is a pan HDAC inhibitor; inhibits HDAC1, HDAC2 and HDAC3 with IC50 values of 9, 9 and 25 nM, respectively.

IC50 & Target

IC50: 9 nM (HDAC1); 9 nM (HDAC2); 25 nM (HDAC3); 6 nM (HDAC6); 107 nM (HDAC8); 72 nM (HDAC10)[1]

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 10mg/kg i.v. HDAC inhibition in PBMCs could not be increased with higher doses up to 50mg/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[1].

In Vivo

Intracellular HDAC inhibition of EDO-S101, which occurs rapidly after dosing is at maximum activity already at the lowest dose of 10mg/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[1].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02576496 Mundipharma-EDO GmbH Hematological Malignancies|Multiple Myeloma|Hodgkin's Lymphoma|Peripheral T-cell Lymphoma|Non-Hodgkin's Lymphoma March 2016 Phase 1
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.4076 mL 12.0378 mL 24.0755 mL
5 mM 0.4815 mL 2.4076 mL 4.8151 mL
10 mM 0.2408 mL 1.2038 mL 2.4076 mL
Kinase Assay
[1]

EDO-S101 is dissolved in DMSO and added to the assay buffer solution. EDO-S101 dilutions of 5 μL of each dilution is added to 50 μL of the reaction mixture including the Fluor de Lys substrate and all of the enzymatic reactions are conducted in duplicate at 37ºC for 30 minutes. After enzymatic reactions, 50 μL of 2xHDAC developer is added to each well and fluorescence intensity is measured[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

EDO-S101 is prepared in PBS.

Rat: The duration of HDAC inhibition is assessed in 12 female rats after receiving a single dose of either vehicle or EDO-S101 (25mg/kg). Blood samples from EDO-S101 treated rats are collected 1hr, 3hr, 6hr, 16hr and 24hr post dosing (n=2 per time point). Blood sample from vehicle treated rats (n=2) are collected 24hr post dosing[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

415.36

Formula

C₁₉H₂₈Cl₂N₄O₂

CAS No.

1236199-60-2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 30 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
EDO-S101
Cat. No.:
HY-101780
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