Valemetostat (DS-3201)

Catalog No.S8926 Batch:S892601

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Technical Data

Formula

C26H34ClN3O4

 
Molecular Weight 488.02 CAS No. 1809336-39-7
Solubility (25°C)* In vitro DMSO 100 mg/mL (204.9 mM)
 
 
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Homogeneous suspension for Oral and Intraperitoneal Injection. Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Valemetostat (DS-3201, DS-3201b) is a selective EZH1/2 dual inhibitor.
Targets
EZH1 [1] EZH2 [1]
In vitro

Valemetostat significantly reducs ATL cell viability compared with the others. Valemetostat significantly reactivates the expression of the highly H3K27me3-accumulated EZH1/2 target genes in an ex vivo culture of primary ATL cells. Valemetostat shows superior anti-growth effects compared with EZH2-selective inhibitor in malignant lymphoma cell lines.[1].

Protocol (from reference)

Selleck's Valemetostat (DS-3201) has been cited by 12 publications

A patient-derived T cell lymphoma biorepository uncovers pathogenetic mechanisms and host-related therapeutic vulnerabilities [ Cell Rep Med, 2025, S2666-3791(25)00102-8] PubMed: 40147445
Targeting USP8 causes synthetic lethality through degradation of FGFR2 in ARID1A-deficient ovarian clear cell carcinoma [ NPJ Precis Oncol, 2025, 9(1):69] PubMed: 40074856
Regulation of chromatin modifications through coordination of nucleus size and epithelial cell morphology heterogeneity [ Commun Biol, 2025, 8(1):269] PubMed: 39979587
Reduced EZH1/2 expression in imipridone-treated cells correlates with synergy following combinations with EZH1/2 or HDAC inhibitors in diffuse glioma and other tumors [ Am J Cancer Res, 2025, 15(3):1307-1320] PubMed: 40226473
Changes in Lysine Methylation Contribute to the Cytotoxicity of Curcumin in Colon Cancer Cells [ Molecules, 2025, 30(2)335] PubMed: 39860204
Lineage-specific canonical and non-canonical activity of EZH2 in advanced prostate cancer subtypes [ Nat Commun, 2024, 15(1):6779] PubMed: 39117665
Inhibiting EZH2 targets atypical teratoid rhabdoid tumor by triggering viral mimicry via both RNA and DNA sensing pathways [ Nat Commun, 2024, 15(1):9321] PubMed: 39472584
A novel EZH1/2 dual inhibitor inhibits GCB DLBCL through cell cycle regulation and M2 tumor-associated macrophage polarization [ J Biol Chem, 2024, 300(11):107788] PubMed: 39303914
Cytotoxicity of bendamustine, alone and in combination with novel agents, toward adult T-cell leukemia cells [ PLoS One, 2024, 19(9):e0309533] PubMed: 39348376
5-AZA Upregulates SOCS3 and PTPN6/SHP1, Inhibiting STAT3 and Potentiating the Effects of AG490 against Primary Effusion Lymphoma Cells [ Curr Issues Mol Biol, 2024, 46(3):2468-2479] PubMed: 38534772

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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