YK-4-279

製品コードS7679 バッチS767903

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C17H13Cl2NO4
分子量 366.20 CAS No. 1037184-44-3
Solubility (25°C)* 体外 DMSO 73 mg/mL (199.34 mM)
Ethanol (warmed with 50ºC water bath) 18 mg/mL (49.15 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.65mg/ml Taking the 1 mL working solution as an example, add 50 μL of 73 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% corn oil
0.6mg/ml Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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 YK-4-279 is a potent inhibitor of EWS-FLI1 binding to RNA helicase A (RHA).
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]

プロトコル(参考用のみ)

キナーゼアッセイ Plasmids and reporter assay
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.

カスタマーフィードバック

Data from [Data independently produced by , , Oncotarget, 2017, 8(55):94780-94792]

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：

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。

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