[CAS NO. 1236199-60-2]  Tinostamustine(EDO-S101)

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PRODUCTS SPECIFICATIONS [1236199-60-2]

Store
Catalog
SLK-S8769
Brand
Selleck
CAS
1236199-60-2

DESCRIPTION [1236199-60-2]

Overview

MDLMFCD28400036
Molecular Weight415.36
Molecular FormulaC19H28Cl2N4O2
SMILESO=C(NO)CCCCCCC1=NC2=CC(N(CCCl)CCCl)=CC=C2N1C

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.4076 mL12.0378 mL24.0755 mL
5 mM0.4815 mL2.4076 mL4.8151 mL
10 mM0.2408 mL1.2038 mL2.4076 mL
50 mM---

Description

Tinostamustine(EDO-S101) is a first-in-class 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


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.