Bulk Inquiry
Valemetostat
- DS-3201B
- Optical Purity: 99% e.e.
- Soluble in DMSO
- MF: C26H34ClN3O4
- MW: 488.02
Description
Valemetostat is an orally available potent and selective inhibitor of EZH1 and EZH2 (the histone lysine methyltransferases enhancer of zeste homolog 1 and 2) (both wild-type and mutated forms) with IC50s in nanomolar concentrations. Demonstrates anti-proliferative effect against various NHL (non-Hodgkin lymphomas) cells, such as diffuse large B-cell lymphoma (DLBCL), mantle cell lymphoma, and peripheral T-cell lymphoma, with GI50 values less than 100 nM regardless of EZH2 gain-of-function mutations; Induces differentiation of undifferentiated NHL cells with increment of cell lineage specific markers and which induced cell death in vitro; Shows synergistic effect with the standard of care agents for NHL in vitro and in vivo.
More Information
| Parent CAS No. | 1809336-39-7 |
|---|---|
| Chemical Name | (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 |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C12O[C@](C)([C@@H]3CC[C@@H](N(C)C)CC3)OC=1C(C)=C(C(NCC1C(=O)NC(C)=CC=1C)=O)C=C2Cl |&1:2,4,7,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C26H34ClN3O4/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/h11-12,17-18H,7-10,13H2,1-6H3,(H,28,31)(H,29,32)/t17?,18?,26-/m1/s1 |
| InChiKey | SSDRNUPMYCFXGM-ZZHSESOFSA-N |
| CID | 126481870 |
| Short Description | EZH1/2 HMTase inhibitor |
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