2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC
  4. Tinostamustine

Tinostamustine  (Synonyms: EDO-S101; NL-101)

Cat. No.: HY-101780 Purity: 99.42%
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Tinostamustine (EDO-S101) est un inhibiteur de pan HDAC; inhibe HDAC6, HDAC1, HDAC2 et HDAC3 avec IC50 valeurs de 9 nM, 9 nM et 25 nM, respectivement.

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.

For research use only. We do not sell to patients.

Tinostamustine Chemical Structure

Tinostamustine Chemical Structure

CAS No. : 1236199-60-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 99 In-stock
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Solid
1 mg USD 50 In-stock
5 mg USD 90 In-stock
10 mg USD 150 In-stock
25 mg USD 280 In-stock
50 mg USD 470 In-stock
100 mg USD 750 In-stock
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Based on 3 publication(s) in Google Scholar

Other Forms of Tinostamustine:

Tinostamustine Related Antibodies

Top Publications Citing Use of Products

View All HDAC Isoform Specific Products:

View All Isoforms
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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)

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]
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]
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.

Tinostamustine Related Antibodies
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
Molecular Weight

415.36

Formula

C19H28Cl2N4O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4076 mL 12.0378 mL 24.0755 mL
5 mM 0.4815 mL 2.4076 mL 4.8151 mL
View the Complete Stock Solution Preparation Table

* 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.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
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].

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].

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

Complete Stock Solution Preparation Table

* 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.

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
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Tinostamustine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tinostamustine1236199-60-2EDO-S101 NL-101NL101NL 101NL-101HDACHistone deacetylasesInhibitorinhibitorinhibit

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