Anticancer agent 304
Anticancer agent 304 is an anticancer agent. Anticancer agent 304 binds to CDC45 with a Kd value of 83.0 μM. Anticancer agent 304 arrests the cell cycle of liver cancer cells at the G2/M phase, induces Apoptosis by upregulating C-PARP-1 and downregulating PARP-1 and BCL-2, and inhibits the migration, invasion and proliferation of liver cancer cells. Anticancer agent 304 suppresses tumor growth in animal models of hepatocellular carcinoma. Anticancer agent 304 is applicable to research related to liver cancer.
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- CAS No.: 3115940-07-0
- Formule: C42H46O8
- Masse moléculaire:678.81
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Anticancer agent 304 (Compound 17) potently inhibits the proliferation of HepG2, Huh-7 and SK-Hep-1 cells, with IC50 values of 1.5 μM, 1.1 μM and 1.1 μM, respectively[1].
Anticancer agent 304 (0.5-1.5 μM; 24 h) inhibits clonogenic proliferation of SK-Hep-1 and Huh-7 cells, reduces the expression level of CDC45 protein in cells, and promotes nuclear export of CDC45 in cells[1].
Anticancer agent 304 (1.56-250 μM) binds directly to purified CDC45 protein, with a Kd of 83.0 μM[1].
Anticancer agent 304 (0.5-1.5 μM; 12 h) arrests SK-Hep-1 and Huh-7 cells at the G2/M phase of the cell cycle by upregulating p27 and downregulating p-CDC2[1].
Anticancer agent 304 (0.5-1.5 μM; 48 h) induces apoptosis in SK-Hep-1 and Huh-7 hepatocellular carcinoma cells by upregulating C-PARP-1 and downregulating PARP-1 and BCL-2[1].
Anticancer agent 304 (0.5-1.5 μM; 48 h) reverses epithelial-mesenchymal transition by upregulating E-cadherin and downregulating N-cadherin and Vimentin, and inhibits the migration and invasion of SK-Hep-1 and Huh-7 hepatocellular carcinoma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Huh-7, SK-Hep-1 hepatocellular carcinoma cell lines
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Concentration:0 μM, 0.5 μM, 1.0 μM, 1.5 μM
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Incubation Time:24 h (initial treatment)
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Result:Inhibited colony formation by 34.0% (0.5 μM), 72.9% (1.0 μM), and 97.6% (1.5 μM) in SK-Hep-1 cells.
Inhibited colony formation by 41.0% (0.5 μM), 64.7% (1.0 μM), and 89.1% (1.5 μM) in Huh-7 cells.
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Cell Line:Huh-7, SK-Hep-1 hepatocellular carcinoma cell lines
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Concentration:0 μM, 0.5 μM, 1.0 μM, 1.5 μM
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Incubation Time:24 h
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Result:Significantly decreased CDC45 protein levels in both Huh-7 and SK-Hep-1 cells.
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Cell Line:Huh-7, SK-Hep-1 hepatocellular carcinoma cell lines
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Concentration:0 μM, 0.5 μM, 1.0 μM, 1.5 μM
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Incubation Time:12 h
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Result:Arrested the cell cycle at the G2/M phase: in SK-Hep-1 cells, the percentage of G2/M phase cells increased from 23.5% to 27.1% (0.5 μM), 41.1% (1.0 μM), and 63.5% (1.5 μM); in Huh-7 cells, the percentage increased from 21.6% to 25.9% (0.5 μM), 28.2% (1.0 μM), and 34.8% (1.5 μM).
Upregulated p27 and downregulated p-CDC2 in both cell lines.
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Cell Line:Huh-7, SK-Hep-1 hepatocellular carcinoma cell lines
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Concentration:0 μM, 0.5 μM, 1.0 μM, 1.5 μM
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Incubation Time:24 h
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Result:Induced nuclear export of CDC45, decreasing nuclear localization and increasing cytoplasmic accumulation in both cell lines.
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Cell Line:Huh-7, SK-Hep-1 hepatocellular carcinoma cell lines
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Concentration:0 μM, 0.5 μM, 1.0 μM, 1.5 μM
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Incubation Time:48 h
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Result:Significantly induced apoptosis: in Huh-7 cells, the proportion of apoptotic cells increased from 4.8% to 14.4% (0.5 μM), 38.5% (1.0 μM), and 72.2% (1.5 μM); in SK-Hep-1 cells, the proportion increased from 2.1% to 28.7% (0.5 μM), 65.5% (1.0 μM), and 84.0% (1.5 μM).
Upregulated C-PARP-1 and downregulated PARP-1 and BCL-2 in both cell lines.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NU/NU nude mice (male, 4 weeks old, subcutaneously injected with Huh-7 cells)[1]
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Dosage:30 mg/kg; 60 mg/kg
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Administration:i.p.; every day; 51 days
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Result:Inhibited tumor growth by 73% at 30 mg/kg after 51 days.
Reduced tumor weight by 76% at 30 mg/kg after 51 days.
Inhibited tumor growth by 84% at 60 mg/kg after 51 days.
Reduced tumor weight by 84% at 60 mg/kg after 51 days.
Reduced CDC45 protein expression in tumor tissues compared to controls.
Caused no compound-related body weight alterations.
Maintained serum levels of hepatic/renal biomarkers (ALT/GPT, AST/GOT, BUN, CRE) within normal ranges.
Showed no structural abnormalities in major organs (heart, liver, spleen, lung, kidney) via histopathological analysis.
Chemical Information
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CAS No. 3115940-07-0
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Masse moléculaire 678.81
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Formule C42H46O8
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SMILES
C[C@@]12C3=C([C@@](O)(CC[C@]4([H])[C@]3([H])OC(C4=C)=O)C)[C@@](C[C@@H]2C(C5=CC=C(C=C5)C([C@@H]6[C@@]7(C8=C([C@@](O)(CC[C@]9([H])[C@]8([H])OC(C9=C)=O)C)[C@](C7)([H])C6)C)=O)=O)([H])C1
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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)
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