2. Cell Cycle/DNA Damage Apoptosis
  3. Topoisomerase Apoptosis Bcl-2 Family
  4. 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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XSJ81

XSJ81 Chemical Structure

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XSJ81 Related Antibodies

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Description

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[1].

IC50 & Target[1]

Topoisomerase I

 

In Vitro

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.

XSJ81 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: DPC-X3 cells
Concentration: 0.35, 0.7, 1.4 μM
Incubation Time: 24 h
Result: Down-regulated S-phase marker CCNA1.
Up-regulated G0/G1-phase regulators CNE1 and P53.

Apoptosis Analysis[1]

Cell Line: DPC-X3 cells
Concentration: 0.35, 0.7, 1.4 μM
Incubation Time: 48 h
Result: Induced dose-dependent apoptosis in DPC-X3 cells.
Up-regulated pro-apoptotic protein BAX.
Down-regulated anti-apoptotic protein Bcl-2.
In Vivo

XSJ81 (100 mg/kg, i.g., single dose, 3-14 days) shows no mortality in 6-week-old female BALB/c mice[1].
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.

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]
Dosage: 5 mg/kg and 10 mg/kg
Administration: i.p., once every 48 h, 14 days
Result: Achieved significant tumor growth inhibition.
Showed no significant changes in body weight.
Induced extensive apoptotic areas in tumor tissues.
Molecular Weight

604.63

Formula

C30H28N4O8S
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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XSJ81 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

XSJ81XSJ 81XSJ-81TopoisomeraseApoptosisBcl-2 Familyampullary carcinomaDPC-X3 cellsInhibitorinhibitorinhibit

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