Anticancer agent 300
Anticancer agent 300 (compound P14) is a CCND1, CDK4, CDK6, and CCNE1 modulator, with anti-proliferative, cell-cycle modulatory, senescence-inducing, and apoptosis-inducing activity. Anticancer agent 300 can be used for the research of ER+/HER2− breast cancer and BRAF-mutant melanoma.
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- No. CAS: 1310059-06-3
- Fòrmula: C24H19N3OS2
- Peso molecular:429.56
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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 300 (P14) (5-50 μM; 7 days) significantly reduces colony-forming capacity in MCF7 and A375 cells and induces cytotoxicity in non-tumoral TC28a2 cells at high concentrations[1].
Anticancer agent 300 (P14) (5-50 μM; 7 days) has an IC50 of 2.018 μM in MCF7 cells and 1.887 μM in A375 cells[1].
Anticancer agent 300 (P14) (5 μM; 12 days) significantly reduces spheroid area in MCF7 and A375 3D cultures[1].
Anticancer agent 300 (P14) (5 μM; 7 days) reduces the proportion of G2/M phase cells in MCF7 and A375 cells[1].
Anticancer agent 300 (P14) (5 μM; 7 days) modulates the expression of cell-cycle-related genes in a cell-type-specific manner, upregulating G1/S transition genes in MCF7 cells and downregulating them in A375 cells[1].
Anticancer agent 300 (P14) (5 μM; 7 days) increases the expression of senescence-associated genes in MCF7 and A375 cells[1].
Anticancer agent 300 (P14) (5 μM; 7 days) upregulates SASP factors in MCF7 cells and reduces their synthesis in A375 cells[1].
Anticancer agent 300 (P14) (5 μM; 7 days) increases cell death and 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
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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. Demonstrated potent anti-proliferative effects even at 5 μM in both cell lines.
Induced cytotoxicity in non-tumoral TC28a2 cells at high concentrations (up to 20 μM).
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Cell Line:MCF7, A375
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Concentration:5, 20, 35, 50 μM
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Incubation Time:7 days
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Result:Achieved an IC50 of 2.018 μM in MCF7 cells and 1.887 μM in A375 cells.
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Cell Line:MCF7, A375
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Concentration:5 μM
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Incubation Time:12 days
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Result:Significantly reduced spheroid area in MCF7 cells after 8 and 12 days of treatment, and in A375 cells with a less marked but still statistically significant reduction.
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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 cells in the G2 phase in both cell lines: decreased MCF7 cells' G2/M phase proportion from 26.25% (control) to 13.10%, and A375 cells' G2/M phase proportion from 5.44% (control) to 0.52%.
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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.
Notably increased the expression of senescence-associated factors, including p21, p53, and p53-responsive genes (IGFBP3 and GDF15), in both cell lines.
Significantly upregulated classical SASP components, including IL-6 and IL-8, in MCF7 cells.
Showed a trend toward reduced synthesis of SASP factors in A375 cells.
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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:Showed a tendency to increase cell death and the proportion of cells undergoing early apoptosis in both cell lines.
Chemical Information
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No. CAS 1310059-06-3
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Peso molecular 429.56
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Fòrmula C24H19N3OS2
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SMILES
C12=C(SC(C3=CC(C4=CC5=C(S4)C=CC=C5)=NC(N6CCOCC6)=N3)=C2)C=CC=C1
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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)
Anticancer agent 300 Related Classifications
HY-181131 Related Classifications
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