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

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

Cat. No.: HY-101780 Purity: 99.42%
COA Handling Instructions

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
Solution
10 mM * 1 mL in DMSO USD 90 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 90 In-stock
Solid
1 mg USD 55 In-stock
5 mg USD 99 In-stock
10 mg USD 165 In-stock
25 mg USD 275 In-stock
50 mg USD 495 In-stock
100 mg USD 825 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

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)

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].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

415.36

Appearance

Solid

Formula

C19H28Cl2N4O2
CAS No.
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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (240.76 mM; Need ultrasonic)

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
10 mM 0.2408 mL 1.2038 mL 2.4076 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

*All of the co-solvents are available by MCE.
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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
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.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Tinostamustine
Cat. No.:
HY-101780
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email address *

Phone number

 

Department *

Organization name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.