XSJ81
XSJ81 is an orally active anti-cancer agent. XSJ81 significantly inhibits the proliferation of ampullary carcinoma (AC) DPC-X3 cells with an IC50 of 0.655 μM. XSJ81 inhibits the colony formation, arrests cell cycle at the G2/M phase and inhibits the migration in DPC-X3 cells. XSJ81 induces DNA damage and apoptosis in DPC-X3 cells. XSJ81 demonstrates significant anti-tumor efficacy in mice bearing DPC-X3 xenografts. XSJ81 can be used for the study of ampullary carcinoma.
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- 화학식: C30H28N4O8S
- 분자량:604.63
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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All Topoisomerase Isoforms
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Biological Activity
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Topoisomerase I |
XSJ81 (0.35-40 μM, 48 h) significantly inhibits the proliferation of ampullary carcinoma (AC) DPC-X3 cells with an IC50 of 0.655 μM[1].
XSJ81 (0.35-1.4 μM, 48 h) dose-dependently reduces EdU fluorescence intensity in DPC-X3 cells[1].
XSJ81 (0.003-0.011 μM, 2 weeks) dose-dependently inhibits the colony formation of DPC-X3 cells[1].
XSJ81 (0.35-1.4 μM, 24-48 h) arrests DPC-X3 cells at the G2/M phase, induces dose-dependent apoptosis and inhibits the migration in DPC-X3 cells[1].
XSJ81 (0.35-1.4 μM, 24 h) induces dose-dependent γ-H2AX foci formation in DPC-X3 cell nuclei[1].
XSJ81 (200-500 μM, 30 min) blocks the relaxation of supercoiled pBR322 plasmid DNA by human Topo I, maintaining the plasmid in a supercoiled form, and promotes proteasomal degradation of Topo I protein[1].
XSJ81 (100-1000 nM, 0-72 h) induces time and dose-dependent cytotoxicity in adenoid cystic carcinoma organoids (ACOs)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DPC-X3 cells
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Concentration:0.35, 0.7, 1.4 μM
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Incubation Time:24 h
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Result:Down-regulated S-phase marker CCNA1.
Up-regulated G0/G1-phase regulators CNE1 and P53.
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Cell Line:DPC-X3 cells
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Concentration:0.35, 0.7, 1.4 μM
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Incubation Time:48 h
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Result:Induced dose-dependent apoptosis in DPC-X3 cells.
Up-regulated pro-apoptotic protein BAX.
Down-regulated anti-apoptotic protein Bcl-2.
XSJ81 (5-10 mg/kg, i.p., once every 48 h, 14 days) demonstrates significant anti-tumor efficacy in nude mice bearing DPC-X3 xenografts[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DPC-X3 cellular suspensions were subcutaneously injected into the right axillary of the nude mice through orthotopic transplantation procedure to construct the DPC-X3 xenograft model[1]
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Dosage:5 mg/kg and 10 mg/kg
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Administration:i.p., once every 48 h, 14 days
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Result:Achieved significant tumor growth inhibition.
Showed no significant changes in body weight.
Induced extensive apoptotic areas in tumor tissues.
Chemical Information
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분자량 604.63
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화학식 C30H28N4O8S
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SMILES
CC[C@]1(C(OC=C2C(N3CC4=CC5=CC=CC=C5N=C4C3CC21)=O)=O)OC(CNC(NS(=O)(C6=CC=C(C=C6)C)=O)=O)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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