CGP 57380

製品コードS7421 バッチS742101

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

C11H9FN6
分子量 244.23 CAS No. 522629-08-9
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 48 mg/mL (196.53 mM)
Water Insoluble
Ethanol 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。

 5.000mg/ml (20.47mM) Taking the 1 mL working solution as an example, add 50 μL of 100 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。

 0.400mg/ml (1.64mM) Taking the 1 mL working solution as an example, add 50 μL of 8 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 CGP 57380 is a potent MNK1 inhibitor with IC50 of 2.2 μM, exhibiting no inhibitory activity on p38, JNK1, ERK1 and -2, PKC, or c-Src-like kinases. CGP 57380 upregulates β-catenin and potentiates radiation-induced apoptosis.
in vitro CGP57380 inhibits phosphorylation of eIF4E in cellular assays with IC50 of about 3 μM. This compound causes dephosphorylation of eIF4E, and induces a further increase in the cap-dependent reporter in 293 cells. [1] It results in dose-dependent decreases in Ang II-stimulated phosphorylation of eIF4E, protein synthesis, and VSMC hypertrophy. [2] This chemical sensitizes wild-type cells for serum-withdrawal induced apoptosis in mouse embryo fibroblasts (MEFs). [3] It prevents the serial replating function of BC progenitors. [4]
in vivo CGP57380 (40 mg/kg/d i.p.) potently extinguishes the ability of BC CML cells to serially transplant-immunodeficient mice and function as LSCs. [4]

プロトコル(参考用のみ)

キナーゼアッセイ In vitro kinase assays
Recombinant p38 isoforms are activated by Mkk6(E) under the following conditions: p38 (100 ng/ml), Mkk6(E) (30 ng/ml), ATP (100 mM) are mixed in kinase buffer (25 mM Hepes, 25 mM b-glycerophosphate, 0.1 mM sodium orthovanadate, 25 mM MgCl2, 2.5 mM DTT, pH 7.4) and incubated for 30 min at 30°C. A typical assay reaction for Mnk1 activity contained Mnk1 (2 ng/ml), HA-eIF4E (10 ng/ml), ATP (300 mM) in kinase buffer. The reaction is started by addition of activated p38 (0.03–3 ng/ml) and stopped after 30 min at 30°C by addition of SDS loading buffer. Inhibitors of Mnk1 are identified under the same assay conditions, except that Mnk1 is pre-activated using active p38a before exposure to the substrate and inhibitors. For radioactive tracer experiments, basically the same reaction conditions are applied, except that the concentrations of Mnk1 and HA-eIF-4E are 10 and 40 ng/ml, respectively. In addition, 1 μCi of [gamma-P33]ATP is added as a radioactive tracer to 20 ml reaction volume. For detection of phosphorylation, an equivalent of the reaction containing 10 ng of HA-eIF4E are subjected to SDS-PAGE and analyzed by Western blotting. For quantitative measurement in ELISA, part of the reaction is diluted with 10 mM Tris-HCl, 50 mM EDTA, pH 7.2 to a concentration of 1.5 ng/ml HA-eIF-4E. 50 ml of this dilution are used to coat a microtiter well. PhosphoeIF-4E is detected using the phospho-specific rabbit antibody, followed by horseradish peroxidase-labeled sheep anti-rabbit antibody. Colorimetric detection is performed using the BM Blue substrate according to the manufacturer’s instructions. In the radioactive tracer experiments, part of the reaction containing 400 ng HA-eIF-4E are used for SDS–PAGE. Incorporation of radioactive label is determined on a PhosphorImager.
動物実験 動物モデル Serial Transplantation Model of Human blast crisis (BC).
投薬量 40 mg/kg/d
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/11463832/
  • https://pubmed.ncbi.nlm.nih.gov/14605021/
  • https://pubmed.ncbi.nlm.nih.gov/17903173/
  • https://pubmed.ncbi.nlm.nih.gov/23737503/

カスタマーフィードバック

Data from [Data independently produced by , , Sci Rep, 2016, 6:18800]

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：

MicroRNA-150-3p enhances the antitumour effects of CGP57380 and is associated with a favourable prognosis in non-small cell lung cancer [ Sci Rep, 2025, 15(1):1973] PubMed: 39809860
25KDa branched polyethylenimine increases interferon-γ production in natural killer cells via improving translation efficiency [ Cell Commun Signal, 2023, 21(1):107] PubMed: 37161542
Inhibition MNK-eIF4E-β-catenin preferentially sensitizes gastric cancer to chemotherapy [ Fundam Clin Pharmacol, 2022, 10.1111/fcp.12759] PubMed: 35048413
EIF4E regulates STEAP1 expression in peritoneal metastasis. [ J Cancer, 2020, 11(4):990-996] PubMed: 31949502
MAP kinase-interacting kinase 1 (MNK1) plays as a tumor suppressor in bladder cancer [ Transl Cancer Res, 2020, 9(4):2588-2598] PubMed: 35117618
Design and synthesis of novel 6-hydroxy-4-methoxy-3-methylbenzofuran-7-carboxamide derivatives as potent Mnks inhibitors by fragment-based drug design. [ Bioorg Med Chem, 2018, 26(16):4602-4614] PubMed: 30115493
eIF4E-phosphorylation-mediated Sox2 upregulation promotes pancreatic tumor cell repopulation after irradiation [Yu Y, et al. Cancer Lett, 2016, 10.1016/j.canlet.2016.02.052] PubMed: 26945967
Dual modulation of Ras-Mnk and PI3K-AKT-mTOR pathways: A Novel c-FLIP inhibitory mechanism of 3-AWA mediated translational attenuation through dephosphorylation of eIF4E. [ur Rasool R, et al. Sci Rep, 2016, 6:18800] PubMed: 26728896

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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