Valemetostat (DS-3201)

製品コードS8926 バッチS892605

印刷

化学情報

Chemical Structure Synonyms DS-3201b Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C26H34ClN3O4

 
分子量 488.02 CAS No. 1809336-39-7
Solubility (25°C)* 体外 DMSO 98 mg/mL (200.81 mM)
Ethanol 49 mg/mL (100.4 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml 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.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 4.900mg/ml (10.04mM) Taking the 1 mL working solution as an example, add 50 μL of 98 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Valemetostat (DS-3201, DS-3201b) is a selective EZH1/2 dual inhibitor.
in vitro

Valemetostat (DS-3201) significantly reducs ATL cell viability compared with the others, significantly reactivates the expression of the highly H3K27me3-accumulated EZH1/2 target genes in an ex vivo culture of primary ATL cells, and shows superior anti-growth effects compared with EZH2-selective inhibitor in malignant lymphoma cell lines.[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 23 cell lines derived from hematological malignancies
濃度
反応時間 1, 7, 14 days
実験の流れ

Valemetostat (DS-3201) is used to treat lymphoma cell models (2 ×105), solid tumor models (1 ×104), and LCLs (2 ×105) plated in 12 well flat bottom plate with optimized medium with 10% of FBS, with simultaneous application of indicated doses of this compound solution in DMSO for 14 days. The cells are maintained by passage into fresh medium every 3 to 4 days. Primary PBMCs from ATL patients (2 ×105 cells/300μL of RPMI1640 with 10% self-serum and 10 ng/ml IL-2) are treated with indicated dose of it for 7 days. The cell numbers are evaluated by Cell Counting Kit-8 following the manufacturer’s protocol. Drug efficacy against HTLV-1 infected population is evaluated by changes of provirus load and phenotypic analysis after 10-12 days treatment.
動物実験 動物モデル DLBCL tumor xenograft
投薬量 100 mg/kg
投与方法 p.o.

参考

  • https://pubmed.ncbi.nlm.nih.gov/31747604/
  • https://www.sciencedirect.com/science/article/pii/S0006497119825892

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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
Valemetostat-SAHA-Driven Acetylation of p53 via SET/TAF-Iβ Displacement and p300 Activation Modulates Cell Cycle Regulators in Pancreatic Cancer Cells [ Biomedicines, 2025, 13(9)2279] PubMed: 41007839
Changes in Lysine Methylation Contribute to the Cytotoxicity of Curcumin in Colon Cancer Cells [ Molecules, 2025, 30(2)335] PubMed: 39860204
EED Maintains the Small Cell Lung Cancer Neuroendocrine Phenotype and Drives Lung Cancer Histological Transformation [ bioRxiv, 2025, 2025.07.07.663486] PubMed: 40672300
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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。