YK-4-279

製品コードS7679 バッチS767901

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) 51 mg/mL (139.26 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.
* <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. This compound also specifically inhibits ESFT cell growth and induces apoptosis. [1] It 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, this compound 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 of this compound. 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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/19584866/
  • https://pubmed.ncbi.nlm.nih.gov/21559405/
  • https://pubmed.ncbi.nlm.nih.gov/25479232/

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：

FLI1 promotes IFN-γ-induced kynurenine production to impair anti-tumor immunity [ Nat Commun, 2024, 15(1):4590] PubMed: 38816360
Deciphering the Metabolic Basis and Molecular Circuitry of the Warburg Paradox in Lymphoma [ Cancers (Basel), 2024, 16(21)3606] PubMed: 39518046
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
Dual functions of SPOP and ERG dictate androgen therapy responses in prostate cancer [ Nat Commun, 2021, 12(1):734] PubMed: 33531470
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

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。