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Synonyms | DS-3201b | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C26H34ClN3O4
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分子量 | 488.02 | CAS No. | 1809336-39-7 | |
Solubility (25°C)* | 体外 | DMSO | 98 mg/mL (200.81 mM) | |
Ethanol | 98 mg/mL (200.81 mM) | |||
Water | Insoluble | |||
* <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. |
製品説明 | Valemetostat (DS-3201, DS-3201b) is a selective EZH1/2 dual inhibitor. |
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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]. |
細胞アッセイ | 細胞株 | 23 cell lines derived from hematological malignancies |
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濃度 | ||
反応時間 | 1, 7, 14 days | |
実験の流れ | Lymphoma cell models (2 ×105), solid tumor models (1 ×104), and LCLs (2 ×105) are plated in 12 well flat bottom plate with optimized medium with 10% of FBS and simultaneously treated with indicated does of 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 inhibitors 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. |
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動物実験 | 動物モデル | DLBCL tumor xenograft |
投薬量 | 100 mg/kg | |
投与方法 | p.o. |
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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 |
Epigenetic plasticity safeguards heterochromatin configuration in mammals [ Nucleic Acids Res, 2023, gkad387] | PubMed: 37178005 |
Exercise-induced histone H3 trimethylation at lysine 27 facilitates the adaptation of skeletal muscle to exercise in mice [ J Physiol, 2022, 600(14):3331-3353] | PubMed: 35666835 |
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。