Apcin

製品コードS9605 バッチS960501

印刷

化学情報

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

C13H14Cl3N7O4
分子量 438.65 CAS No. 300815-04-7
Solubility (25°C)* 体外 DMSO 88 mg/mL (200.61 mM)
Ethanol 10 mg/mL (22.79 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.
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。

 4.000mg/ml (9.12mM) Taking the 1 mL working solution as an example, add 50 μL of 80 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。

 6.600mg/ml (15.05mM) Taking the 1 mL working solution as an example, add 50 μL of 132 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 Apcin (APC inhibitor) is an inhibitor of the E3 ligase activity of the mitotic anaphase-promoting complex/cyclosome (APC/C) that binds to Cdc20 and competitively inhibits the ubiquitylation of D-box-containing substrates.
in vitro

Apcin is a novel cell‑permeable molecule that blocks the interaction between APC/C and Cdc20. This compound is demonstrated to inhibit OS cell growth and induce significant apoptosis. The invasion and mobile abilities of OS cells are also markedly suppressed by this chemical treatment. Furthermore, Bim and p21 are upregulated in OS cells following this treatment.[2] The inhibition of CDC20 with its inhibitor Apcin reduces the adhesion rate and proliferation ability to RL95-2 and HEC-1A cells, respectively.[3]
in vivo

CDC20 inhibitor Apcin inhibits embryo implantation in vivo.[3]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Human osteosarcoma cell lines MG63 and U2OS
濃度 25 μM, 50 μM, 75 μM
反応時間 24 h, 48 h, 72 h
実験の流れ

MG63 and U2OS (2.5×103 cells/well) are seeded in 96‑well plates and cultured overnight. Different concentrations of apcin are added to the medium and cultured for 24, 48 and 72 h, respectively. An MTT assay is then carried out to assess the cell viability according to the manufacturer's protocols. Then, 10 μl of MTT solution (0.5 mg/ml) is added to each well followed by incubation for 4 h. The liquid supernatant is then drained off and 100 μl of DMSO is added to each well to dissolve the crystals. The absorbance of each well at 490 nm is determined using a Multimode Reader of SpectraMax M5.
動物実験 動物モデル 8-week-old adult C57BL/6 female mice (weighing 20 to 25 g), 12-week-old adult C57BL/6 male mice (weighing 40 to 50 g)
投薬量 --
投与方法 Uterine horn injection

参考

  • https://pubmed.ncbi.nlm.nih.gov/25156254/
  • https://pubmed.ncbi.nlm.nih.gov/29901174/
  • https://pubmed.ncbi.nlm.nih.gov/32458533/

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：

The formation and propagation of human Robertsonian chromosomes [ Nature, 2025, 647(8091):952-961] PubMed: 40993387
A novel pathway for stemness propagation and chemoresistance in non-small cell lung cancer via phosphorylated PKM2-loaded small extracellular vesicles [ Theranostics, 2025, 15(8):3439-3461] PubMed: 40093893
CDC20 protects the heart from doxorubicin-induced cardiotoxicity by modulating CCDC69 degradation [ Cell Mol Biol Lett, 2025, 30(1):29] PubMed: 40045239
p53 directly downregulates the expression of CDC20 to exert anti-tumor activity in mantle cell lymphoma [ Exp Hematol Oncol, 2023, 12(1):28] PubMed: 36882855
Inhibition of Cdc20 suppresses the metastasis in triple negative breast cancer (TNBC) [ Breast Cancer, 2021, 10.1007/s12282-021-01242-z] PubMed: 33813687
Molecular response to PARP1 inhibition in ovarian cancer cells as determined by mass spectrometry based proteomics [ J Ovarian Res, 2021, 14(1):140] PubMed: 34686201
Androgen receptor negatively regulates mitotic checkpoint signaling to induce docetaxel resistance in castration-resistant prostate cancer [ Prostate, 2021, 10.1002/pros.24257] PubMed: 34672379

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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