受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C11H9FN6 |
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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) |
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* <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. |
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. |
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in vitro | CGP57380 inhibits phosphorylation of eIF4E in cellular assays with IC50 of about 3 μM. CGP57380 causes dephosphorylation of eIF4E, and induces a further increase in the cap-dependent reporter in 293 cells. [1] CGP57380 results in dose-dependent decreases in Ang II-stimulated phosphorylation of eIF4E, protein synthesis, and VSMC hypertrophy. [2] CGP57380 sensitizes wild-type cells for serum-withdrawal induced apoptosis in mouse embryo fibroblasts (MEFs). [3] CGP57380 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] |
キナーゼアッセイ | In vitro kinase assays | |
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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. |
Data from [Data independently produced by , , Sci Rep, 2016, 6:18800]
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 |
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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