Anticancer agent 314
Anticancer agent 314 is a multi-target anticancer agent with tubulin polymerization inhibitory activity (IC50 = 6.35 μM) and human carbonic anhydrase IX (Ki = 27.1 nM) and XII (Ki 20.9 = nM) inhibitory activity. Anticancer agent 314 binds to the colchicine-binding pocket of tubulin and inhibits tumor-associated carbonic anhydrase isoforms via zinc coordination within enzyme active sites. Anticancer agent 314 induces G2/M phase cell cycle arrest, apoptosis via p53-dependent signaling, and broad-spectrum antiproliferative activity across multiple cancer cells. Anticancer agent 314 can be used for the research of cancer, such as leukemia, melanoma, ovarian cancer.
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- Formule: C22H16N6O4S
- Masse moléculaire:460.47
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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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hCA XII 20.9 nM (Ki) |
hCA IX 27.1 nM (Ki) |
Anticancer agent 314 (Compound 13n) potently inhibits the recombinant human tumor-associated carbonic anhydrase isoforms hCA IX (Ki = 27.1 nM) and hCA XII (Ki = 20.9 nM)[1].
Anticancer agent 314 (1.5-100 μM) potently inhibits cell-free tubulin polymerization with an IC50 of 6.35 μM[1].
Anticancer agent 314 (0.01-100 μM) exhibits broad-spectrum antiproliferative activity across the NCI-60 human tumor cell line panel, with GI50 values ranging from 2.48 to 31.00 μM[1].
Anticancer agent 314 has low cytotoxicity against WI-38 normal human lung fibroblasts, with an IC50 of 68.62 μM[1].
Anticancer agent 314 (6.35 μM; 24 h) potently arrests MCF-7 human breast cancer cells in the G2/M phase of the cell cycle, increasing the G2/M population to 31.97%[1].
Anticancer agent 314 (6.35 μM; 24 h) induces robust apoptosis in MCF-7 human breast cancer cells, increasing the total apoptotic population to 24.68%[1].
Anticancer agent 314 (6.35 μM; 24 h) activates the p53-dependent apoptotic pathway in MCF-7 human breast cancer cells, increasing p53, Bax, and activated caspase-7 levels while reducing Bcl-2 levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 human breast cancer cells
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Concentration:6.35 μM
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Incubation Time:24 h
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Result:Increased the G2/M phase population from 13.81% (control) to 31.97% (treated).
Suppressed the G0/G1 phase population from 63.58% to 52.76%.
Reduced the S phase population from 22.61% to 15.27%.
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Cell Line:MCF-7 human breast cancer cells
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Concentration:6.35 μM
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Incubation Time:24 h
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Result:Increased the total apoptotic cell population from 0.67% (control) to 24.68% (treated), with 9.51% early apoptotic cells and 15.17% late apoptotic cells.
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Cell Line:MCF-7 human breast cancer cells
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Concentration:6.35 μM
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Incubation Time:24 h
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Result:Increased p53 protein levels 3.43-fold relative to control cells.
Increased Bax levels 12.34-fold relative to control cells.
Reduced Bcl-2 levels 4.37-fold relative to control cells.
Increased caspase-7 activation 7.35-fold relative to control cells.
Chemical Information
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Masse moléculaire 460.47
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Formule C22H16N6O4S
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SMILES
CC1=NN2C(C3=CC4=C(OC3=O)C=CC=C4)=CC=NC2=C1/N=N/C5=CC=C(C=C5)S(N)(=O)=O
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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)
Anticancer agent 314 Related Classifications
HY-182245 Related Classifications
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- Anticancer agent 314
- Anticancer agent314
- Anticancer agent-314
- Microtubule/Tubulin
- Carbonic Anhydrase
- Apoptosis
- MDM-2/p53
- human carbonic anhydrase XII
- colchicine-binding pocket
- melanoma
- p53-dependent signaling
- ovarian cancer
- G2/M phase cell cycle arrest
- leukemia
- tubulin polymerization
- human carbonic anhydrase IX
- MCF-7 human breast cancer cells
- Inhibitor
- inhibitor
- inhibit