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Background Information:
Valemetostat (DS-3201) (DS-3201b) (Optically Pure) 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. It is currently in clinical development for treatment of AML (Acute Myelogenous Leukemia), ALL (Acute Lymphocytic Leukemia) and B-cell and T-cell NHL (ref. 1).
Reference:
1. D. Honma, et al, DS-3201, a Potent EZH1/2 Dual Inhibitor, Demonstrates Antitumor Activity Against Non-Hodgkin Lymphoma (NHL) Regardless of EZH2 Mutation, ASH Annual Meeting, December 1, 2018, https://ash.confex.com/ash/2018/webprogram/Paper113379.html.
APIM050068: VALEMETOSTAT (DS-3201) (DS-3201B)
CAS No.: 1809336-39-7.
Molecular Formula: C26H34ClN3O4.
Molecular Weight: 488.0 (Refer to Certificate of Analysis, batch-specific).
Purity: 99.9-100% by achiral and chiral HPLCs.
QC: Achiral and Chiral HPLCs, NMR, and Quantitative Elemental Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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