Anticancer agent 299
Anticancer agent 299 (compound P12) is a cell-cycle inhibitor, senescence inducer, apoptosis inducer, and antiproliferative agent. Anticancer agent 299 exhibits selective activity against cancer cells with minimal effects on non-tumoral chondrocyte cells at relevant concentrations. Anticancer agent 299 can be used for the research of ER+/HER2− breast cancer and BRAF-mutant melanoma.
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- No. CAS: 1414873-26-9
- Fòrmula: C25H20F3N3O
- Peso molecular:435.44
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
Anticancer agent 299 (P12) (5-50 μM; 7 days) reduces colony-forming capacity in MCF7 and A375 cells with IC50 values of 30.22 μM and 2.915 μM, respectively, and has minimal effect on non-tumoral TC28a2 cells at 5-35 μM[1].
Anticancer agent 299 (P12) (5 μM; 12 days MCF7 treatment, 4 days A375 measurement) reduces spheroid area in MCF7 cells after 8 and 12 days and in A375 cells after 4 days[1].
Anticancer agent 299 (P12) (5 μM; 7days) reduces the proportion of G2/M phase cells in MCF7 (to 15.65%) and A375 (to 1.94%) cells[1].
Anticancer agent 299 (P12) (5 μM; 7 days) upregulates G1/S and S-phase entry genes in MCF7 cells and downregulates those genes in A375 cells[1].
Anticancer agent 299 (P12) (5 μM; 7 days) increases the expression of senescence-associated genes (p21, p53, IGFBP3, GDF15) in MCF7 and A375 cells[1].
Anticancer agent 299 (P12) (5 μM; 7 days) upregulates SASP factors (IL-6, IL-8) in MCF7 cells but not in A375 cells[1].
Anticancer agent 299 (P12) (≥4 days) increases early apoptosis in MCF7 and A375 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF7, A375, TC28a2
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Concentration:5, 20, 35, 50 μM (MCF7, A375 colony formation); 5, 20, 35, 50 μM (TC28a2 viability assay)
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Incubation Time:7 days
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Result:Significantly reduced the colony-forming capacity of MCF7 and A375 cells in a dose-dependent manner. Achieved an IC50 of 30.22 μM in MCF7 cells and 2.915 μM in A375 cells. Did not produce a significant reduction in the number of adherent viable cells in non-tumoral TC28a2 cells from 5 to 35 μM.
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Cell Line:MCF7, A375
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Concentration:5 μM
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Incubation Time:12 days (MCF7 treatment); 4 days (A375 measurement)
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Result:Significantly reduced spheroid area of MCF7 cells compared with the untreated control after 8 and 12 days of treatment. Significantly reduced spheroid size of A375 cells after 4 days of culture.
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Cell Line:MCF7, A375
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Concentration:5 μM
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Incubation Time:7 days
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Result:Reduced the proportion of G2/M phase cells to 15.65% in MCF7 cells (vs. 26.25% untreated) and to 1.94% in A375 cells (vs. 5.44% untreated).
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Cell Line:MCF7, A375
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Concentration:5 μM
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Incubation Time:7 days
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Result:Significantly upregulated genes associated with G1/S transition and S-phase entry in MCF7 cells. Significantly downregulated key regulators of the G1/S transition and S-phase entry, including CCND1, CDK4, CDK6, and CCNE1, in A375 cells.\nInduced a notable increase in the expression of senescence-associated factors, including p21, p53, IGFBP3, and GDF15, in both MCF7 and A375 cells.\nSignificantly upregulated classical SASP components including IL-6 and IL-8 in MCF7 cells. Did not induce SASP factor expression and showed a trend toward reduced synthesis in A375 cells.
Chemical Information
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No. CAS 1414873-26-9
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Peso molecular 435.44
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Fòrmula C25H20F3N3O
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SMILES
FC(F)(C1=CC=C(C=C1)C2=CC(C3=CC=CC4=C3C=CC=C4)=NC(N5CCOCC5)=N2)F
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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