Evo312
Evo312 is a dose-dependent inhibitor of protein kinase CβⅠ (PKCβⅠ) (IC50 is 117.34 nM). Evo312 induces PANC-GR (acquired gemcitabine-resistant PC cells) cell cycle arrest and apoptosis by inhibiting PKCβ1 protein expression. Evo312 has antiproliferative effects in pancreatic cancer cells PANC-1 and PANC-GR cells with IC50 of 0.08 μM and 0.07 μM, and in human normal pancreatic ductal epithelial cells HPDE6-c7 with IC50 of 2.95 μM. Evo312 exhibits antitumor activity in a PANC-GR cell transplantation mouse model.
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- CAS No.: 2820245-53-0
- Formule: C21H19N3O3
- Masse moléculaire:361.39
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Activité biologique
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PKC-βI 117.34 nM (IC50) |
Evo312 (0-160 nM, 24 h) inhibits PKCβ1 protein expression and downstream target protein phosphorylation in PANC-GR cells[1].
Evo312 (0-160 nM, 24 h) induces G2/M cell cycle arrest in PANC-GR cells, inhibiting to cell mitosis[1].
Evo312 (0-160 nM, 48 h) induces apoptosis in PANC-GR cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PANC-GR (an acquired gemcitabine-resistant PC cell line, cell line PANC-GR was established in vitro from PANC-1 cells by exposing gemcitabine with gradually increasing concentrations (0.1−2 μM))
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Concentration:0, 40, 80, 160 nM
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Incubation Time:24 h
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Result:Increased the number of G2/M cells from 37.53% to 58.51%, leading to mitosis.
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Cell Line:PANC-GR, PANC-1
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Concentration:40, 80, 160 nM
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Incubation Time:48 h
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Result:Increased total cell death (including early apoptosis, late apoptosis and necrosis) by 15.83%, 20.63% and 24.95%.
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Cell Line:PANC-GR, PANC-1
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Concentration:0, 40, 80, 160 nM
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Incubation Time:24 h; 48 h
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Result:Inhibited the expression of PKCβ1 protein at 24 h, and inhibited the phosphorylation of glycogen synthase kinase 3β (GSK3β), protein kinase B (Akt), signal transducer and activator of transcription 5 (STAT5), and ribosomal protein S6 kinase β-1 (70S6K) in a dose-dependent manner.
Downregulated the expression levels of CDK (CDK2 and cdc2) and cyclin D1 proteins at 24 h, while upregulated the expression levels of cyclin B1 and p27 proteins.
Increased the expression levels of apoptosis markers caspase3, caspase8, and caspase9 proteins at 48 h.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:PANC-GR cell mouse xenograft model; PANC-1 cell mouse xenograft model[1]
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Dosage:40 mg/kg; 5 mg/kg, three times a week, 20 days
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Administration:Intraperitoneal injection (i.p.)
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Result:Did not cause mouse death or significant toxicity at a dose of 40 mg/kg. At a dose of 5 mg/kg, the tumor volume was inhibited by 72%, and the tumor weight was reduced by 44.89% compared with the drug-loaded treatment group, with no significant toxicity or weight changes, and the expression of PKCβI in tumor tissues implanted with PANC-GR cells was effectively inhibited.
Chemical Information
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CAS No. 2820245-53-0
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Masse moléculaire 361.39
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Formule C21H19N3O3
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SMILES
O=C1C2=C(N(C3N1CCC4=C3NC5=CC=C(OC(C)=O)C=C45)C)C=CC=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Evo312 Related Classifications
HY-169006 Related Classifications
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