Tinostamustine(EDO-S101)

Catalog No.S8769

For research use only.

Tinostamustine(EDO-S101) is a first-in-class alkylating deacetylase inhibitor with IC50 values of 9 nM, 9 nM, 25 nM and 107 nM for HDAC1, HDAC2, HDAC3 and HDAC8 (Class 1 HDACs) respectively and 6 nM, 72 nM for HDAC6 and HDAC10 (Class II HDACs).

Tinostamustine(EDO-S101) Chemical Structure

CAS No. 1236199-60-2

Purity & Quality Control

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Biological Activity

Description Tinostamustine(EDO-S101) is a first-in-class alkylating deacetylase inhibitor with IC50 values of 9 nM, 9 nM, 25 nM and 107 nM for HDAC1, HDAC2, HDAC3 and HDAC8 (Class 1 HDACs) respectively and 6 nM, 72 nM for HDAC6 and HDAC10 (Class II HDACs).
Targets
HDAC6 [1]
(Cell-free assay)
HDAC1 [1]
(Cell-free assay)
HDAC2 [1]
(Cell-free assay)
HDAC3 [1]
(Cell-free assay)
HDAC10 [1]
(Cell-free assay)
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6 nM 9 nM 9 nM 25 nM 72 nM
In vitro

The IC50s of EDO-S101 range between 5-13 μM in 8 myeloma cell lines. EDO-S101 has significant synergistic cytotoxicity with the proteasome inhibitors bortezomib and carfilzomib across all cell types tested. EDO-S101 induces strong protein and histone acetylation and is a strong inducer of pIRE-1, the key activator protein of the UPR in MM cells[2].

Assay
Methods Test Index PMID
Western blot pATR / pCHK1 / pATM / pCHK2 / p53 / γH2AX ; Ac-H3 / Ac-H4 / Ac α-tubulin ; caspase-8 / caspase-9 / caspase-7 / caspase-3 / PARP ; AIF / COX IV ; NOXA / p-MCL1 / p-S-BCL2 / BCL2 28633670 28753594
Immunofluorescence γH2AX / Rad51 28633670
Growth inhibition assay Cell viability 28633670

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: HL-60 cells
  • Concentrations: 4 μM
  • Incubation Time: 0, 6, 12, 18, 24h
  • Method:

    --

Animal Research:

[1]

  • Animal Models: subcutaneous Daudi human Burkitt's lymphoma xenograft model
  • Dosages: 39 and 78 mg/kg
  • Administration: i.v.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 415.36
Formula

C19H28Cl2N4O2

CAS No. 1236199-60-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C2=C(C=C(C=C2)N(CCCl)CCCl)N=C1CCCCCCC(=O)NO

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03903458 Recruiting Drug: Tinostamustine Malignant Melanoma Markus Joerger|Cantonal Hospital of St. Gallen March 7 2019 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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