Art. -Nr.: HY-101780

Tinostamustine

(Synonyms: EDO-S101; NL-101)

5 Cited Publications

Kundenbewertung

Based on 5 publication(s) in Google Scholar

Tinostamustine (EDO-S101) is a pan HDAC inhibitor; inhibits HDAC6, HDAC1, HDAC2 and HDAC3 with IC₅₀ values of 6 nM, 9 nM, 9 nM and 25 nM, respectively.

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Reinheit: 99.64%
CAS. Nr.: 1236199-60-2
Formel: C₁₉H₂₈Cl₂N₄O₂
Molecular Weight:415.36

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Tinostamustine Chemical Structure

CAS. Nr.: 1236199-60-2

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (5)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Tinostamustine (EDO-S101) is a pan HDAC inhibitor; inhibits HDAC6, HDAC1, HDAC2 and HDAC3 with IC₅₀ values of 6 nM, 9 nM, 9 nM and 25 nM, respectively^[1].

IC₅₀ & Target^[1]

HDAC6

6 nM (IC₅₀)

HDAC1

9 nM (IC₅₀)

HDAC2

9 nM (IC₅₀)

HDAC3

25 nM (IC₅₀)

HDAC10

72 nM (IC₅₀)

HDAC8

107 nM (IC₅₀)

Alle HDAC Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Kasumi 1	IC₅₀	820 nM Compound: 22	Cytotoxicity against human Kasumi 1 cells assessed as inhibition of cell growth by MTT assay Cytotoxicity against human Kasumi 1 cells assessed as inhibition of cell growth by MTT assay	[PMID: 32791404]
MEF	IC₅₀	5700 nM Compound: 9	Antiproliferative activity against mouse MEF cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against mouse MEF cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 37989059]
NB-4	IC₅₀	900 nM Compound: 22	Cytotoxicity against human NB-4 cells assessed as inhibition of cell growth by MTT assay Cytotoxicity against human NB-4 cells assessed as inhibition of cell growth by MTT assay	[PMID: 32791404]
NCI-H460	IC₅₀	2200 nM Compound: 9	Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay	[PMID: 37989059]
Panel NCI-60 (60 carcinoma cell lines)	IC₅₀	2.2 μM Compound: 162	Cytotoxicity against human Panel NCI-60 (60 carcinoma cell lines) Cytotoxicity against human Panel NCI-60 (60 carcinoma cell lines)	[PMID: 33077264]

In Vitro

Tinostamustine 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. Tinostamustine 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Intracellular HDAC inhibition of Tinostamustine, 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 Tinostamustine 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 Tinostamustine^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1236199-60-2
Appearance Solid
Molecular Weight 415.36
Formel C₁₉H₂₈Cl₂N₄O₂
Color White to off-white
SMILES

O=C(NO)CCCCCCC1=NC2=CC(N(CCCl)CCCl)=CC=C2N1C
Synonyms

EDO-S101; NL-101
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (5)

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Journal Impact Factor

Acta Pharmacol Sin

P300/CBP inhibition sensitizes mantle cell lymphoma to PI3Kδ inhibitor idelalisib. [Abstract]

2022 Feb;43(2):457-469. PMID: 33850273
Nutrients

Butyrate Protects Barrier Integrity and Suppresses Immune Activation in a Caco-2/PBMC Co-Culture Model While HDAC Inhibition Mimics Butyrate in Restoring Cytokine-Induced Barrier Disruption. [Abstract]

2023 Jun 15;15(12):2760. PMID: 37375664
Int J Mol Sci

Tinostamustine (EDO-S101) and Its Combination with Celecoxib or Temozolomide as a Therapeutic Option for Adult-Type Diffuse Gliomas. [Abstract]

2025 Jan 14;26(2):661. PMID: 39859375
Int J Mol Sci

Butyrate Prevents Induction of CXCL10 and Non-Canonical IRF9 Expression by Activated Human Intestinal Epithelial Cells via HDAC Inhibition. [Abstract]

2022 Apr 2;23(7):3980. PMID: 35409339
Int J Parasitol Drugs Drug Resist

2026 May 17;31:100649.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (240.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (6.02 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

Tinostamustine is dissolved in DMSO and added to the assay buffer solution. Tinostamustine 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 37°C for 30 minutes. After enzymatic reactions, 50 μL of 2xHDAC developer is added to each well and fluorescence intensity is measured^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Rats: The duration of HDAC inhibition is assessed in 12 female rats after receiving a single dose of either vehicle or Tinostamustine (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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Mehrling T, et al. The Alkylating-HDAC Inhibition Fusion Principle: Taking Chemotherapy to the Next Level with the First in Class Molecule EDO-S101. Anticancer Agents Med Chem. 2016;16(1):20-8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4076 mL	12.0378 mL	24.0755 mL	60.1888 mL
	5 mM	0.4815 mL	2.4076 mL	4.8151 mL	12.0378 mL
	10 mM	0.2408 mL	1.2038 mL	2.4076 mL	6.0189 mL
	15 mM	0.1605 mL	0.8025 mL	1.6050 mL	4.0126 mL
	20 mM	0.1204 mL	0.6019 mL	1.2038 mL	3.0094 mL
	25 mM	0.0963 mL	0.4815 mL	0.9630 mL	2.4076 mL
	30 mM	0.0803 mL	0.4013 mL	0.8025 mL	2.0063 mL
	40 mM	0.0602 mL	0.3009 mL	0.6019 mL	1.5047 mL
	50 mM	0.0482 mL	0.2408 mL	0.4815 mL	1.2038 mL
	60 mM	0.0401 mL	0.2006 mL	0.4013 mL	1.0031 mL
	80 mM	0.0301 mL	0.1505 mL	0.3009 mL	0.7524 mL
	100 mM	0.0241 mL	0.1204 mL	0.2408 mL	0.6019 mL

Keywords

Tinostamustine

5 Cited Publications

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Tinostamustine

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Publications Citing Use of MedChemExpress (MCE) Tinostamustine

Alle HDAC Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tinostamustine

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Rare Diseases Drug Library

Anti-Pulmonary Fibrosis Compound Library

Osteogenesis Compound Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Tinostamustine

Alle HDAC Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tinostamustine Related Classifications

HY-101780 Related Classifications