Tinostamustine(EDO-S101)

Catalog No.S8769 Batch:S876901

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Technical Data

Formula

C19H28Cl2N4O2
Molecular Weight 415.36 CAS No. 1236199-60-2
Solubility (25°C)* In vitro DMSO 14 mg/mL (33.7 mM)
Ethanol 2 mg/mL (4.81 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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)		 View More
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].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    HL-60 cells

  • Concentrations

    4 μM

  • Incubation Time

    0, 6, 12, 18, 24h

  • Method

    --
Animal Study:

[1]
  • Animal Models

    subcutaneous Daudi human Burkitt's lymphoma xenograft model

  • Dosages

    39 and 78 mg/kg

  • Administration

    i.v.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.