DS-3201
DS-3201 Basic information
- Product Name:
- DS-3201
- Synonyms:
-
- 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
- CAS:
- 1809336-39-7
- MF:
- C26H34ClN3O4
- MW:
- 488.02
- Mol File:
- 1809336-39-7.mol
DS-3201 Chemical Properties
- 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
DS-3201 Usage And Synthesis
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
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