Valemetostat tosylate
- Product Name
- Valemetostat tosylate
- CAS No.
- 1809336-93-3
- Chemical Name
- Valemetostat tosylate
- Synonyms
- DS-3201 tosylate;Valemetostat tosylate;Valemetostat tosylayte;Valemetostat 4-methylbenzenesulfonic acid;(2R)-7-chloro-2-[trans-4-(dimethylamino)cyclohexyl]-N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-2,4-dimethyl-1,3-benzodioxole-5-carboxamide tosylate;(R)-7-Chloro-N-[(4,6-dimethyl-2-oxo-1,2-dihydro-3-pyridyl)methyl]-2-[trans-4-(dimethylamino)cyclohexyl]-2,4-dimethylbenzo[d][1,3]dioxole-5-carboxamide Tosylate;(R)-7-Chloro-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-(trans-4-(dimethylamino)cyclohexyl)-2,4-dimethylbenzo[d][1,3]dioxole-5-carboxamide 4-methylbenzenesulfonate
- CBNumber
- CB85821314
- Molecular Formula
- C33H42ClN3O7S
- Formula Weight
- 660.22
- MOL File
- 1809336-93-3.mol
Valemetostat tosylate Property
- storage temp.
- Store at -20°C
- solubility
- DMSO: 125 mg/mL (189.33 mM)
- form
- Solid
- color
- White to yellow
N-Bromosuccinimide Price
- Product number
- CS-0101884
- Product name
- Valemetostat(tosylate)
- Purity
- 99.91%
- Packaging
- 5mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CS-0101884
- Product name
- Valemetostat(tosylate)
- Purity
- 99.91%
- Packaging
- 10mg
- Price
- $550
- Updated
- 2021/12/16
- Product number
- CS-0101884
- Product name
- Valemetostat(tosylate)
- Purity
- 99.91%
- Packaging
- 25mg
- Price
- $990
- Updated
- 2021/12/16
- Product number
- CS-0101884
- Product name
- Valemetostat(tosylate)
- Purity
- 99.91%
- Packaging
- 50mg
- Price
- $1650
- Updated
- 2021/12/16
- Product number
- CS-0101884
- Product name
- Valemetostat(tosylate)
- Purity
- 99.91%
- Packaging
- 100mg
- Price
- $2250
- Updated
- 2021/12/16
Valemetostat tosylate Chemical Properties,Usage,Production
Uses
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].
in vivo
Valemetostat tosylate (0.01 mg/g; i.p.; once) prevents the changes of H3K27me3 after exercise training[2].
| 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. |
IC 50
EZH1
References
[1] Daiichi Sankyo’s EZH1/2 Dual Inhibitor Valemetostat (DS-3201) Receives SAKIGAKE Designation for Treatment of Patients with Relapsed/Refractory Peripheral T-Cell Lymphoma from Japan MHLW.
[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. DOI:10.1113/JP282917
[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. DOI:10.1016/j.celrep.2019.10.083
Valemetostat tosylate Preparation Products And Raw materials
Raw materials
Preparation Products
Valemetostat tosylate Suppliers
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