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

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Valemetostat tosylate Property

storage temp.: Store at -20°C
solubility: DMSO: 125 mg/mL (189.33 mM)
form: Solid
color: White to yellow

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0101884
Product name: Valemetostat(tosylate)
Purity: 99.91%
Packaging: 5mg
Price: $350
Updated: 2021/12/16

ChemScene

Product number: CS-0101884
Product name: Valemetostat(tosylate)
Purity: 99.91%
Packaging: 10mg
Price: $550
Updated: 2021/12/16

ChemScene

Product number: CS-0101884
Product name: Valemetostat(tosylate)
Purity: 99.91%
Packaging: 25mg
Price: $990
Updated: 2021/12/16

ChemScene

Product number: CS-0101884
Product name: Valemetostat(tosylate)
Purity: 99.91%
Packaging: 50mg
Price: $1650
Updated: 2021/12/16

ChemScene

Product number: CS-0101884
Product name: Valemetostat(tosylate)
Purity: 99.91%
Packaging: 100mg
Price: $2250
Updated: 2021/12/16

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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

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1809336-93-3, Valemetostat tosylateRelated Search:

Valemetostat tosylate

DS-3201 tosylate

Valemetostat tosylayte

(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

(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

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

1809336-93-3