OTS514 hydrochloride

製品コードS7652 バッチS765201

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

C21H20N2O2S.HCl
分子量 400.92 CAS No. 2319647-76-0
Solubility (25°C)* 体外 DMSO 80 mg/mL (199.54 mM)
Water 80 mg/mL (199.54 mM)
Ethanol 5 mg/mL (12.47 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.
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 (9.98mM)
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。

 0.650mg/ml (1.62mM)
* <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 OTS514 is a highly potent TOPK(T-LAK cell-originated protein kinase) inhibitor with an IC50 value of 2.6 nM. OTS514 induces cell cycle arrest and apoptosis.
in vitro OTS514 has growth inhibitory effect on five kidney cancer cell lines, VMRC-RCW, Caki-1, Caki-2, 769-P and 786-O, in which TOPK was highly expressed. The IC50 values range from 19.9 to 44.1 nM[1]. OTS514 strongly suppressed the growth of TOPK-positive cancer cells. It also shows significant growth-inhibitory effect on ovarian cancer cell lines with IC50 values of 3.0 to 46 nM[3].
in vivo Mouse xenograft studies with human lung cancer cells demonstrated the in vivo efficacy of OTS514 but found that the compound also caused severe hematopoietic toxicity [reduction of red blood cells (RBCs) and white blood cells (WBCs) associated with marked increase in platelets][2]. Oral administration of OTS514 significantly elongated overall survival in the ES-2 abdominal dissemination xenograft model, compared with vehicle control (P < 0.001)[3].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 CD34+ HSCs
濃度 20 or 40 nM
反応時間 48 h
実験の流れ Cells were cultured in RPMI supplemented with 20% fetal bovine serum and 1×StemSpan CC100. Cells were treated with OTS514 (20 or 40 nM) or OTS964 (100 or 200 nM) for 48 hours. Collected cells were washed with PBS and resuspended in 100 ml of PBS followed by staining with CD41a antibody for 20 min at room temperature. Finally, the cells were washed with PBS again and then analyzed for CD41a staining by flow cytometry. Expression of STAT5 was examined by Western blot with an anti-STAT5 antibody.
動物実験 動物モデル BALB/cSLC-nu/nu mice
投薬量 1, 2.5, and 5 mg/kg
投与方法 IV or oral gavage

参考

  • https://pubmed.ncbi.nlm.nih.gov/26933922/
  • https://pubmed.ncbi.nlm.nih.gov/25338756/
  • https://pubmed.ncbi.nlm.nih.gov/27334838/

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：

PBK drives PARP inhibitor resistance through the TRIM37/NFκB axis in ovarian cancer [ Exp Mol Med, 2022, 54(7):999-1010] PubMed: 35859118
T-LAK cell-originated protein kinase (TOPK): an emerging prognostic biomarker and therapeutic target in osteosarcoma [ Mol Oncol, 2021, 15(12):3721-3737] PubMed: 34115928
PBK phosphorylates MSL1 to elicit epigenetic modulation of CD276 in nasopharyngeal carcinoma [ Oncogenesis, 2021, 10(1):9] PubMed: 33431797
PBK Enhances Cellular Proliferation With Histone H3 Phosphorylation and Suppresses Migration and Invasion With CDH1 Stabilization in Colorectal Cancer [ Front Pharmacol, 2021, 12:772926] PubMed: 35115926
PBK expression predicts favorable survival in colorectal cancer patients [ Virchows Arch, 2021, 10.1007/s00428-021-03062-0] PubMed: 33638656
T-LAK cell-originated protein kinase (TOPK) is a Novel Prognostic and Therapeutic Target in Chordoma [ Cell Prolif, 2020, e12901] PubMed: 32960500
PBK promotes aggressive phenotypes of cervical cancer through ERK/c-Myc signaling pathway [ J Cell Physiol, 2020, 10.1002/jcp.30134] PubMed: 33184870
Novel Interleukin-6 Inducible Gene PDZ-Binding Kinase Promotes Tumor Growth of Multiple Myeloma Cells [ J Interferon Cytokine Res, 2020, 40(8):389-405] PubMed: 32721246
TOPKi-NBD: a fluorescent small molecule for tumor imaging. [ Eur J Nucl Med Mol Imaging, 2019, 10.1007/s00259-019-04608-w] PubMed: 31734783
PBK, targeted by EVI1, promotes metastasis and confers cisplatin resistance through inducing autophagy in high-grade serous ovarian carcinoma [ Cell Death Dis, 2019, 10(3):166] PubMed: 30778048

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。