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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C17H13Cl2NO4 |
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分子量 | 366.20 | CAS No. | 1037184-44-3 | |
Solubility (25°C)* | 体外 | DMSO | 73 mg/mL (199.34 mM) | |
Ethanol | 73 mg/mL warmed with 50ºC water bath (199.34 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 | YK-4-279 is a potent inhibitor of EWS-FLI1 binding to RNA helicase A (RHA). |
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in vitro | YK-4-279 eliminates cyclin D levels by blocking the interaction of EWS-FLI1 with RHA in EWS-FLI1-containing TC32 cells. YK-4-279 also specifically inhibits ESFT cell growth and induces apoptosis. [1] YK-4-279 also inhibits ERG and ETV1 biological activity in fusion-positive prostate cancer cells, and further decreases cell motility and invasion. [2] |
in vivo | In vivo, YK-4-279 (1.5 mg/dose i.p.) inhibits the growth of ESFT xenograft tumors. [1] In mouse model, YK-4-279 selectively prevents prostate cancer growth and metastasis in fusion-positive LNCaP-luc-M6 tumors. [3] |
キナーゼアッセイ | Plasmids and reporter assay | |
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The NR0B131 luciferase reporter and full-length EWS-FLI1 are transiently transfected into COS-7 cells with Fugene-6 and luciferase assay performed per manufacturer's protocol (Dual Luciferase Kit). Six hours following transfection, cells are treated with either 3 or 10 μM YK-4-279. Cell lysates luciferase activity levels are standardized to renilla activity from a non-affected promoter and plotted as relative luciferase activity (RLA). | ||
動物実験 | 動物モデル | Nude mice bearing prostate cancer PC3, TC71 or CHP-100 xenografts |
投薬量 | 1.5 mg/dose | |
投与方法 | i.p. |
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Data from [Data independently produced by , , Oncotarget, 2017, 8(55):94780-94792]
High-Content and High-Throughput Clonogenic Survival Assay Using Fluorescence Barcoding [ Cancers -Basel), 2023, 15(19)4772] | PubMed: 37835466 |
TK216 targets microtubules in Ewing sarcoma cells [ Cell Chem Biol, 2022, 29(8):1325-1332.e4] | PubMed: 35803262 |
The ETS Inhibitor YK-4-279 Suppresses Thyroid Cancer Progression Independent of TERT Promoter Mutations [ Front Oncol, 2021, 11:649323] | PubMed: 34221969 |
Telomerase Reverse Transcriptase Promoter Mutations Identify a Genomically Defined and Highly Aggressive Human Pleural Mesothelioma Subgroup [ Clin Cancer Res, 2020, 26(14):3819-3830] | PubMed: 32317288 |
Telomerase Reverse Transcriptase Promoter Mutations Identify a Genomically Defined and Highly Aggressive Human Pleural Mesothelioma Subgroup [ Clin Cancer Res, 2020, 21;clincanres35732019] | PubMed: 32317288 |
p53 Loss Mediates Hypersensitivity to ETS Transcription Factor Inhibition Based on PARylation-Mediated Cell Death Induction [ Cancers (Basel), 2020, 12(11)E3205] | PubMed: 33143299 |
Gene Essentiality Profiling Reveals Gene Networks and Synthetic Lethal Interactions with Oncogenic Ras. [ Cell, 2019, 36(2):179-193] | PubMed: 28162770 |
A Pharmacogenomic Landscape in Human Liver Cancers. [ Cancer Cell, 2019, 36(2):179-193] | PubMed: 31378681 |
Antiviral candidates against the hepatitis E virus (HEV) and their combinations inhibit HEV growth in in vitro. [ Antiviral Res, 2019, 170:104570] | PubMed: 31362004 |
TERT expression is susceptible to BRAF and ETS-factor inhibition in BRAFV600E/TERT promoter double-mutated glioma. [ Acta Neuropathol Commun, 2019, 7(1):128] | PubMed: 31391125 |
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。