Valemetostat tosylate
Based on 5 publication(s) in Google Scholar
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.
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- Purity : 99.84%
- CAS No.: 1809336-93-3
- 화학식: C33H42ClN3O7S
- 분자량:660.22
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Valemetostat tosylate
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Customer Validation & Images
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RT-PCR
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Cell Proliferation/Viability Assay
All Histone Methyltransferase Isoforms
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Biological Activity
제품 설명
IC50 & Target
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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.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J mice with chronic and acute running exercise or without exercise[1]
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Dosage:0.01 mg/g
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Administration:Intraperitoneal injection; 0.01 mg/g; 30 min before the start of running exercise
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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
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1809336-93-3
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Appearance Solid
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분자량 660.22
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화학식 C33H42ClN3O7S
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Color White to yellow
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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
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Synonyms
DS-3201 tosylate
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (5)
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Journal Impact Factor
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Most Recent
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Cancer Res
2025 May 15;85(10):1803-1818. PMID: 39992701
Valemetostat tosylate purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 May 15;85(10):1803-1818. [Abstract]
qRT-PCR showing SMARCA4 and ARHGAP29 levels in NTC cells and SMARCA4 KD cells treated with EZH inhibitors with corresponding concentration. Valemetostat (0.1 μM; 10 d) restored ARHGAP29 expression in SMARCA4 knockdown cells.
Valemetostat tosylate purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 May 15;85(10):1803-1818. [Abstract]
Valemetostat (0.1-1 μM; 12 d) partially reversed the growth-promoting effects of SMARCA4 knockdown.
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Protein Cell
2025 Jun 20;16(6):439-457. PMID: 39945726 -
Cells
Characterization of a Preclinical In Vitro Model Derived from a SMARCA4-Mutated Sinonasal Teratocarcinosarcoma. [Abstract]2023 Dec 30;13(1):81. PMID: 38201285 -
Am J Pathol
Toll-Interacting Protein Down-Regulation by Cigarette Smoke Exposure Impairs Human Lung Defense against Influenza A Virus Infection. [Abstract]2025 Jun;195(6):1124-1140. PMID: 40056974 -
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (277 KB)
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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)
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Handling Instructions (2659 KB)
References
[2]. Shimizu J, Kawano F. Exercise-induced histone H3 trimethylation at lysine 27 facilitates the adaptation of skeletal muscle to exercise in mice. J Physiol. 2022 Jul;600(14):3331-3353. [Content Brief]
[3]. Yamagishi M, et al. Targeting Excessive EZH1 and EZH2 Activities for Abnormal Histone Methylation and Transcription Network in Malignant Lymphomas. Cell Rep. 2019 Nov 19;29(8):2321-2337.e7. [Content Brief]
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 |
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| 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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