SC66

製品コードS5313 バッチS531301

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

C18H16N2O

分子量 276.33 CAS No. 871361-88-5
Solubility (25°C)* 体外 DMSO 55 mg/mL (199.03 mM)
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.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

1.25mg/ml (4.52mM) Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of 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

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

1.25mg/ml (4.52mM) Taking the 1 mL working solution as an example, add 50 μL of 25 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 SC66 is an allosteric inhibitor which displays a dual-inhibitory function toward AKT activity with IC50 values of 0.77, 2.85 and 0.47 μg/ml in HepG2, Huh7 and Hep3B cells after 72 h treatment, respectively.
in vitro SC66 reduces cell viability in a dose- and time-dependent manner, inhibits colony formation and induces apoptosis in HCC cells. This compound treatment leads to a reduction in total and phospho-AKT levels. This is associated with alterations in cytoskeleton organization, a reduction in expression levels of E-cadherin, β-catenin and phospho-FAK, together with up-regulation of Snail protein levels. In addition, it induces the production of reactive oxygen species (ROS) and DNA damage. It affects AKT/mTOR signaling in HCC cell lines[1].
in vivo In the mouse xenograft tumor model of Hep3B cells, SC66 treatment significantly reduces tumor volume to 37% on day 17 of treatment when compared with tumors in the untreated group. The inhibition of cell growth correlates with a reduction in phospho-AKT levels in the tumors of animals treated with this compound[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 The human hepatocarcinoma cell lines HepG2, Huh7, PLC/PRF/5, Hep3B and HA22T/VGH cells
濃度 2 and 4 μg/ml
反応時間 1, 3 and 6 hours
実験の流れ Caspase activity assays: Cells (2 × 104/well) are treated with 2 and 4 μg/ml SC66 and after 1, 3 and 6 hours the levels of caspase3/7 activities in the cells are measured by the Caspase-Glo® 3/7 Assay. Results are expressed as relative luminescence units (RLU). Values are the mean ± SD of two separate experiments, each performed in duplicate.
動物実験 動物モデル Male nude athymic mice (Fox1 nu/nu) aged 4 weeks inoculated with Hep3B cells at the right flank
投薬量 5 and 25 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/25596737/

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:

Dexmedetomidine facilitates autophagic flux to promote liver regeneration by suppressing GSK3β activity in mouse partial hepatectomy [ Biomed Pharmacother, 2024, 177:117038] PubMed: 39002441
Inhibition of autophagy can promote the apoptosis of bladder cancer cells induced by SC66 through the endoplasmic reticulum stress pathway [ Chem Biol Interact, 2023, 10.1016/j.cbi.2023.110725] PubMed: 37741534
SC66 inhibits the proliferation and induces apoptosis of human bladder cancer cells by targeting the AKT/β-catenin pathway [ J Cell Mol Med, 2021, 10.1111/jcmm.17005] PubMed: 34687144
[ Oncol Lett, 2020, ] PubMed: 32863924
Targeting Akt by SC66 triggers GSK-3β mediated apoptosis in colon cancer therapy. [ Cancer Cell Int, 2019, 19:124] PubMed: 31168297
Allosteric AKT Inhibitors Target Synthetic Lethal Vulnerabilities in E-Cadherin-Deficient Cells. [ Cancers (Basel), 2019, 11(9)] PubMed: 31540244
Transformation of normal cells by aberrant activation of YAP via cMyc with TEAD. [ Sci Rep, 2019, 9(1):10933] PubMed: 31358774

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。