Valemetostat tosylayte
Valemetostat, also known as DS-3201 is a potent, selective and orally active EZH1/2 inhibitor. DS-3201 selectively inhibits the activity of both wild-type and mutated forms of EZH1 and EZH2. Inhibition of EZH1/2 specifically prevents the methylation of lysine 27 on histone H3 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways, enhances transcription of certain target genes, and results in decreased proliferation of EZH1/2-expressing cancer cells.
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Chemical Information
| Name | Valemetostat tosylayte |
|---|---|
| Iupac Chemical Name | (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 |
| Synonyms | Valemetostat tosylayte; Valemetostat; DS-3201; DS 3201; DS3201; DS-3201b |
| Molecular Formula | C33H42ClN3O7S |
| Molecular Weight | 660.22 |
| Smile | O=C(C1=CC(Cl)=C(O[C@](C)([C@H]2CC[C@H](N(C)C)CC2)O3)C3=C1C)NCC4=C(C)C=C(C)NC4=O.OS(=O)(C5=CC=C(C)C=C5)=O |
| InChiKey | JSBKGJUYSLVFPF-WJQUPPJOSA-N |
| InChi | InChI=1S/C26H34ClN3O4.C7H8O3S/c1-14-11-15(2)29-25(32)20(14)13-28-24(31)19-12-21(27)23-22(16(19)3)33-26(4,34-23)17-7-9-18(10-8-17)30(5)6;1-6-2-4-7(5-3-6)11(8,9)10/h11-12,17-18H,7-10,13H2,1-6H3,(H,28,31)(H,29,32);2-5H,1H3,(H,8,9,10)/t17-,18-,26-;/m1./s1 |
| CAS Number | 1809336-93-3 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| HS Code |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
Yamagishi M, Hori M, Fujikawa D, et al. Targeting Excessive EZH1 and EZH2 Activities for Abnormal Histone Methylation and Transcription Network in Malignant Lymphomas. Cell Rep. 2019;29(8):2321–2337.e7. doi:10.1016/j.celrep.2019.10.083
Chemical Structure
