YCJ-02
YCJ-02 is a selective Topoisomerase I (Top I) inhibitor. YCJ-02 can inhibit cell proliferation and induce apoptosis and G2/M phase arrest. YCJ-02 can induce DNA damage and increaseγ-H2AX levels. YCJ-02 can promote Top I deqradation via a ubiquitin/26S proteasome pathway. YCJ-02 increases the expressions of pro-apoptotic proteins Bad, Bax, and cleaved caspase-3. YCJ-02 shows broad-spectrum antitumor activity. YCJ-02 can be used for the research of cancer, such as intrahepatic cholangiocarcinoma (ICC).
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- CAS No.: 2260557-09-1
- Formule: C23H19F2N3O3
- Masse moléculaire:423.41
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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
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Topoisomerase I |
YCJ-02 shows antitumor activities in HepG2, HuCCT1, BXPC-3, SW1990, HCT-116, SW480, A2780, HeLa, and MCF-7 cells with IC50 values of 0.025, 0.079, 1.15, 0.20, 0.16, 0.12, 0.25, 0.79, and 1.08 μM, respectively[1].
YCJ-02 inhibits proliferation in human HuCCT1, RBE, QBC-939, and mouse A/N, B/R ICC cells with IC50 values of 0.079, 0.31, 0.35, 1.51, and 2.68 μM, respectively[1].
YCJ-02 (0.25-1 μM, 72 h) inhibits colony formation in QBC-939 and HuCCT1 cells[1].
YCJ-02 (0.25-1 μM, 24-48 h) induces G2/M phase arrest and apoptosis in QBC-939 and HuCCT1 cells[1].
YCJ-02 (0.05-0.8 μM) dose-dependently inhibits the Top I enzyme activity and exhibits minimal inhibitory activity against Top II[1].
YCJ-02 (0.125-1 μM, 48 h) reduces Top I levels in QBC-939 and HuCCT1 cells[1].
YCJ-02 (0.125-1 μM, 48 h) induces DNA damage[1].
YCJ-02 (0.125-1 μM) reduced the levels of AKT, p-AKTser473, mTORC1, p-mTORC1ser2448, and Notch1 (NICD) in QBC-939 and A/N cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:QBC-939 and HuCCT1 cells
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Concentration:0.25, 0.5 and 1μM
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Incubation Time:24 and 48 h
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Result:Increased apoptotic rates.
Upregulated levels of p21, p53 and Bcl-2.
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Cell Line:QBC-939 and HuCCT1 cells
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Concentration:0.125, 0.25, 0.5 and 1μM
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Incubation Time:48 h
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Result:Reduced Top I levels.
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Cell Line:QBC-939 cells
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Concentration:0.125, 0.25, 0.5 and 1μM
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Incubation Time:12 h
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Result:Reduced Top I levels.
Increased γ-H2AX levels.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:AKT/NICD-induced primary ICC mice models[1]
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Dosage:10 mg/kg
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Administration:Intraperitoneally injection, 2 weeks for 10 times
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Result:Reduced tumor volume and prolonged survival.
Had no significant body weight loss.
Decreased tumor area.
Reduced the positive cell rates of CK19 and Ki-67.
Reduced Top I levels and increased the levels of p21, p53, cleaved caspase 3, and γ-H2AX.
Reduced p-AKTser473, mTORC1, p-mTORC1ser2448, and Notch1 (NICD).
Chemical Information
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CAS No. 2260557-09-1
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Masse moléculaire 423.41
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Formule C23H19F2N3O3
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SMILES
O=C1C2=CC(F)=C(C=C2C3=C(N1CCN4CCCC4)C5=CC6=C(OCO6)C=C5N=C3)F
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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)
YCJ-02 Related Classifications
HY-175700 Related Classifications
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