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Tinostamustine(EDO-S101) HDAC inhibitor

Name: Tinostamustine(EDO-S101)
Brand: Selleck Chemicals
SKU: S8769
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S8769

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 and 72 nM for HDAC6 and HDAC10 (Class II HDACs).

Chemical Structure

Molecular Weight: 415.36

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Quality Control

Batch: S876901 DMSO]14 mg/mL]false]Ethanol]2 mg/mL]false]Water]Insoluble]false Purity: 99.7%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.7

Related Targets	JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Other HDAC Inhibitors	ITF-2357 (Givinostat) Hydrochloride Monohydrate Fimepinostat (CUDC-907) Trichostatin A (TSA) Entinostat (MS-275) RGFP966 Quisinostat (JNJ-26481585) Dihydrochloride Tubastatin A HCl Tubastatin A Mocetinostat (MGCD0103) Ricolinostat (ACY-1215)

Solubility

In vitro
Batch:

DMSO : 14 mg/mL (33.7 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

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% DMSO

% Tween 80

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	415.36	Formula	C₁₉H₂₈Cl₂N₄O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1236199-60-2	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CN1C2=C(C=C(C=C2)N(CCCl)CCCl)N=C1CCCCCCC(=O)NO

Mechanism of Action

Targets/IC₅₀/Ki	HDAC6 (Cell-free assay) 6 nM HDAC1 (Cell-free assay) 9 nM HDAC2 (Cell-free assay) 9 nM HDAC3 (Cell-free assay) 25 nM HDAC10 (Cell-free assay) 72 nM HDAC8 (Cell-free assay) 107 nM
In vitro	In 8 myeloma cell lines, the IC50s of Tinostamustine (EDO-S101) range between 5–13 μM. It has significant synergistic cytotoxicity with the proteasome inhibitors bortezomib and carfilzomib across all cell types tested. This compound induces strong protein and histone acetylation and is a strong inducer of pIRE-1, the key activator protein of the UPR in MM cells.
References	[1] https://pubmed.ncbi.nlm.nih.gov/25980817/ [2] http://www.bloodjournal.org/content/124/21/2249?sso-checked=true

Applications

Methods	Biomarkers	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
Immunofluorescence	γH2AX / Rad51	28633670
Growth inhibition assay	Cell viability	28633670