2. Epigenetics
  3. Histone Methyltransferase
  4. Valemetostat tosylate

Valemetostat tosylate  (Synonyms: DS-3201 tosylate)

Cat. No.: HY-109108A Purity: 98.14%
COA Handling Instructions

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Valemetostat (DS-3201) tosylate, a first-in-class EZH1/2 dual inhibitor with IC50 values ＜10 nM. Valemetostat tosylate can be used for the research of relapsed/refractory peripheral T-cell lymphoma.

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

Valemetostat tosylate Chemical Structure

Valemetostat tosylate Chemical Structure

CAS No. : 1809336-93-3

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1 mg USD 119 In-stock
5 mg USD 250 In-stock
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25 mg USD 798 In-stock
50 mg USD 1135 In-stock
100 mg USD 1800 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Valemetostat tosylate:

Valemetostat tosylate Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Valemetostat tosylate

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Valemetostat (DS-3201) tosylate, a first-in-class EZH1/2 dual inhibitor with IC50 values ＜10 nM. Valemetostat tosylate can be used for the research of relapsed/refractory peripheral T-cell lymphoma[1][2][3].

IC50 & Target

EZH1

 

In Vitro

Valemetostat tosylate (1-1000 nM) strongly and specifically inhibits EZH1 and EZH2 with IC50 values ＜10 nM[3].
Valemetostat tosylate (100 nM; 7 d) effectively removes H3K27me3 and also prevents unexpected gain of H3K27me3[3].
Valemetostat tosylate (0.1-100 nM; 7 d) potently inhibits H3K27me3 by low-dose treatment in the sensitive lymphoma types[3].

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

Valemetostat tosylate Related Antibodies
In Vivo

Valemetostat tosylate (0.01 mg/g; i.p.; once) prevents the changes of H3K27me3 after exercise training[2].

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

Animal Model: Male C57BL/6J mice with chronic and acute running exercise or without exercise[1]
Dosage: 0.01 mg/g
Administration: Intraperitoneal injection; 0.01 mg/g; 30 min before the start of running exercise
Result: Significantly increased the level of H3K27me3 , slightly decresed EZH1 level , upregulated the EZH2 level and increased the level of phosphorylated AMPK after exercise. Repressed myonuclear H3K27me3 accumulation during training and caused a failure of adaptive changes.
Clinical Trial
Molecular Weight

660.22

Formula

C33H42ClN3O7S
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=S(C1=CC=C(C)C=C1)(O)=O.CC2=C(O[C@@](C)([C@]3([H])CC[C@@H](N(C)C)CC3)O4)C4=C(Cl)C=C2C(NCC(C5=O)=C(C=C(C)N5)C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (151.46 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 1.5146 mL 7.5732 mL 15.1465 mL
5 mM 0.3029 mL 1.5146 mL 3.0293 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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: ≥ 2.08 mg/mL (3.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (3.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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

Purity: 98.14%

COA (251 KB) HNMR (303 KB) RP-HPLC (245 KB)

Handling Instructions (2659 KB)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5146 mL 7.5732 mL 15.1465 mL 37.8662 mL
5 mM 0.3029 mL 1.5146 mL 3.0293 mL 7.5732 mL
10 mM 0.1515 mL 0.7573 mL 1.5146 mL 3.7866 mL
15 mM 0.1010 mL 0.5049 mL 1.0098 mL 2.5244 mL
20 mM 0.0757 mL 0.3787 mL 0.7573 mL 1.8933 mL
25 mM 0.0606 mL 0.3029 mL 0.6059 mL 1.5146 mL
30 mM 0.0505 mL 0.2524 mL 0.5049 mL 1.2622 mL
40 mM 0.0379 mL 0.1893 mL 0.3787 mL 0.9467 mL
50 mM 0.0303 mL 0.1515 mL 0.3029 mL 0.7573 mL
60 mM 0.0252 mL 0.1262 mL 0.2524 mL 0.6311 mL
80 mM 0.0189 mL 0.0947 mL 0.1893 mL 0.4733 mL
100 mM 0.0151 mL 0.0757 mL 0.1515 mL 0.3787 mL
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Valemetostat tosylate 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:

Valemetostat1809336-93-3DS-3201DS3201DS 3201Histone MethyltransferaseT-cell leukemiadual inhibitorInhibitorinhibitorinhibit

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