受注:045-509-1970 |
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Synonyms | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C20H25N5O3 |
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分子量 | 383.44 | CAS No. | 1616391-65-1 | |
Solubility (25°C)* | 体外 | DMSO | 77 mg/mL warmed with 50ºC water bath (200.81 mM) | |
Ethanol | 26 mg/mL warmed with 50ºC water bath (67.8 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 | EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs. |
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in vitro | EPZ015666 shows potent cellular activity that blocks symmetric dimethylation of SmD3 and inhibit proliferation of MCL cell lines (Z-138, Granta-519, Maver-1, Mino, and Jeko-1) with IC50 of 96-904 nM. [1] |
in vivo | EPZ015666 (200 mg/kg, p.o.) displays robust anti-tumor activity in MCL xenograft animal models. [1] |
細胞アッセイ | 細胞株 | MCL cell lines (Z-138, Granta-519, Maver-1, Mino, and Jeko-1) |
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濃度 | 5 μM | |
反応時間 | 12 days | |
実験の流れ | -- |
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動物実験 | 動物モデル | MCL (Z-138, and Maver-1) xenograft models |
投薬量 | 200 mg/kg BID | |
投与方法 | p.o. |
Data from [Data independently produced by , , J Cell Mol Med, 2016, 1-10.]
Genome-wide mapping of cancer dependency genes and genetic modifiers of chemotherapy in high-risk hepatoblastoma [ Nat Commun, 2023, 14(1):4003] | PubMed: 37414763 |
FACS-based genome-wide CRISPR screens define key regulators of DNA damage signaling pathways [ Mol Cell, 2023, 83(15):2810-2828.e6] | PubMed: 37541219 |
PRMT blockade induces defective DNA replication stress response and synergizes with PARP inhibition [ Cell Rep Med, 2023, 4(12):101326] | PubMed: 38118413 |
Inhibition of histone methyltransferase PRMT5 attenuates cisplatin-induced hearing loss through the PI3K/Akt-mediated mitochondrial apoptotic pathway [ J Pharm Anal, 2023, 13(6):590-602] | PubMed: 37440906 |
(S)-2-(Cyclobutylamino)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)isonicotinamide Attenuates RANKL-Induced Osteoclast Differentiation by Inhibiting NF-κB Nuclear Translocation [ Int J Mol Sci, 2023, 24(5)4327] | PubMed: 36901758 |
SHARPIN Enhances Ferroptosis in Synovial Sarcoma Cells via NF-κB- and PRMT5-Mediated PGC1α Reduction [ Cancers (Basel), 2023, 15(13)3484] | PubMed: 37444594 |
PRMT5/FGFR3/AKT Signaling Axis Facilitates Lung Cancer Cell Metastasis [ Technology in Cancer Research & Treatment, 2023, 10.1177/15330338231161139] | PubMed: None |
PRMT5/FGFR3/AKT Signaling Axis Facilitates Lung Cancer Cell Metastasis [ Technol Cancer Res Treat, 2023, 22:15330338231161139] | PubMed: 36927233 |
The Spliceosome: A New Therapeutic Target in Chronic Myeloid Leukaemia [ Cancers (Basel), 2022, 14(19)4695] | PubMed: 36230624 |
PRMT5 Promotes Cyclin E1 and Cell Cycle Progression in CD4 Th1 Cells and Correlates With EAE Severity [ Front Immunol, 2021, 12:695947] | PubMed: 34168658 |
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。