ChemicalBook > CAS DataBase List > DS-3201

DS-3201

Product Name: DS-3201
CAS No.: 1809336-39-7
Chemical Name: DS-3201
Synonyms: DS-3201;Valemetostat;Valemetostat (DS-3201);Valemetostat, 10 mM in DMSO;Valemetostat (DS-3201) ，S8926;VALEMETOSTAT (DS-3201) (DS-3201B);Desmopressin Impurity 3 (Desmopressin EP Impurity C);inhibit,DS 3201,DS3201,Histone Methyltransferase,Inhibitor,T-cell,Valemetostat,lymphoma;(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;1,3-Benzodioxole-5-carboxamide, 7-chloro-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-2-[trans-4-(dimethylamino)cyclohexyl]-2,4-dimethyl-, (2R)-
CBNumber: CB24806093
Molecular Formula: C26H34ClN3O4
Formula Weight: 488.02
MOL File: 1809336-39-7.mol

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DS-3201 Property

Boiling point:: 610.0±55.0 °C(Predicted)
Density: 1.26±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO: soluble
form: A crystalline solid
pka: 11.87±0.10(Predicted)
color: White to off-white
InChIKey: SSDRNUPMYCFXGM-UYPAYLBCSA-N
SMILES: O1C2=C(Cl)C=C(C(NCC3=C(C)C=C(C)NC3=O)=O)C(C)=C2O[C@]1([C@@H]1CC[C@@H](N(C)C)CC1)C

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Hazard and Precautionary Statements (GHS)

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DS-3201 Chemical Properties,Usage,Production

Uses

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

in vivo

Valemetostat (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

DS-3201 Preparation Products And Raw materials

Raw materials

Preparation Products

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1809336-39-7, DS-3201Related Search:

DS-3201

(R)-7-chloro-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-((1r,4R)-4-(dimethylamino)cyclohexyl)-2,4-dimethylbenzo[d][1,3]dioxole-5-carboxamide

Valemetostat

1,3-Benzodioxole-5-carboxamide, 7-chloro-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-2-[trans-4-(dimethylamino)cyclohexyl]-2,4-dimethyl-, (2R)-

inhibit,DS 3201,DS3201,Histone Methyltransferase,Inhibitor,T-cell,Valemetostat,lymphoma

Valemetostat (DS-3201)

VALEMETOSTAT (DS-3201) (DS-3201B)

(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

Desmopressin Impurity 3 (Desmopressin EP Impurity C)

Valemetostat, 10 mM in DMSO

Valemetostat (DS-3201) ，S8926

1809336-39-7

809336-39-7

C26H34ClN3O4