Anticancer agent 357
Anticancer agent 357 is an orally active HER2 inhibitor. Anticancer agent 357 reduces the phosphorylation levels of HER2, AKT and GSK-3β, and downregulates the expression of β-catenin. Anticancer agent 357 inhibits the proliferation and migration of colon cancer cells with high HER2 expression, and suppresses tumor growth in xenograft models. Anticancer agent 357 can be used in colorectal cancer-related research.
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- Fòrmula: C20H15F3N4
- Peso molecular:368.36
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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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HER2 |
GSK-3β |
Akt |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCM460 | IC50 |
38.62 μM
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Inhibition of cell viability against human normal colon epithelial NCM460 cells incubated for 24 hrs by CCK-8 assay.
Inhibition of cell viability against human normal colon epithelial NCM460 cells incubated for 24 hrs by CCK-8 assay.
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42492133 |
| LS174T | IC50 |
24.17 μM
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Inhibition of cell viability against human colon cancer LS174T cells incubated for 24 hrs by CCK-8 assay.
Inhibition of cell viability against human colon cancer LS174T cells incubated for 24 hrs by CCK-8 assay.
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42492133 |
| HCT-116 | IC50 |
29.74 μM
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Inhibition of cell viability against human colon cancer HCT116 cells incubated for 24 hrs by CCK-8 assay.
Inhibition of cell viability against human colon cancer HCT116 cells incubated for 24 hrs by CCK-8 assay.
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42492133 |
| NCM460 | IC50 |
21.18 μM
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Inhibition of cell viability against human normal colon epithelial NCM460 cells incubated for 72 hrs by CCK-8 assay.
Inhibition of cell viability against human normal colon epithelial NCM460 cells incubated for 72 hrs by CCK-8 assay.
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42492133 |
| LS174T | IC50 |
9.57 μM
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Inhibition of cell viability against human colon cancer LS174T cells incubated for 72 hrs by CCK-8 assay.
Inhibition of cell viability against human colon cancer LS174T cells incubated for 72 hrs by CCK-8 assay.
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42492133 |
| HCT-116 | IC50 |
9.71 μM
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Inhibition of cell viability against human colon cancer HCT116 cells incubated for 72 hrs by CCK-8 assay.
Inhibition of cell viability against human colon cancer HCT116 cells incubated for 72 hrs by CCK-8 assay.
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42492133 |
Anticancer agent 357 (compound 7) (0-40 μM; 24-72 h) inhibits the viability of LS174T and HCT116 colon cancer cells as well as NCM460 normal colonic epithelial cells in a dose- and time-dependent manner; after 72 h of incubation, its potency and selectivity against colon cancer cells are enhanced (IC50 values: 9.57 μM for LS174T cells, 9.71 μM for HCT116 cells)[1].
Anticancer agent 357 (20 μM; 24-48 h) significantly inhibits the proliferation and migration of LS174T and HCT116 colon cancer cells, as detected by scratch wound healing assay[1].
Anticancer agent 357 (30 μM; 0-24 h) inhibits the HER2/AKT/GSK-3β/β-catenin signaling pathway in LS174T and HCT116 colon cancer cells by reducing the phosphorylation levels of HER2, AKT and GSK-3β, and downregulating β-catenin protein expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human colon cancer LS174T cells, human colon cancer HCT116 cells, human normal colon epithelial NCM460 cells
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Concentration:0, 1.5, 2.5, 5, 10, 20, 40 μM
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Incubation Time:24 h; 48 h; 72 h
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Result:Inhibited cell viability in all three cell lines in a concentration- and time-dependent manner.
Exhibited 24 h IC50 values of 38.62 μM (NCM460), 24.17 μM (LS174T), and 29.74 μM (HCT116).
Exhibited 72 h IC50 values of 21.18 μM (NCM460), 9.57 μM (LS174T), and 9.71 μM (HCT116).
Achieved selectivity index (SI) of 1.60 for LS174T and 1.30 for HCT116 at 24 h, and increased to 2.21 for LS174T and 2.18 for HCT116 at 72 h.
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Cell Line:human colon cancer LS174T cells, human colon cancer HCT116 cells
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Concentration:20 μM
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Incubation Time:24 h
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Result:Markedly inhibited migratory capacity of LS174T and HCT116 cells.
Resulted in significantly lower percent wound closure in both cell lines relative to the vehicle control.
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Cell Line:human colon cancer LS174T cells, human colon cancer HCT116 cells
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Concentration:20 μM
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Incubation Time:48 h
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Result:Suppressed colony formation by LS174T and HCT116 cells.
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Cell Line:human colon cancer LS174T cells, human colon cancer HCT116 cells
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Concentration:30 μM
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Incubation Time:0, 2, 3, 4 h (HER2/AKT analysis)
0, 6, 9, 12 h (GSK-3β analysis)
24 h (β-catenin analysis) -
Result:Induced a time-dependent reduction in phosphorylation of HER2 (Tyr1221/1222) and AKT (Ser473) in both cell lines.
Caused a time-dependent decrease in phosphorylation of GSK-3β (Ser9) in both cell lines.
Downregulated β-catenin protein expression significantly in both cell lines after 24 h treatment relative to the control.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (4-6 weeks old)[1]
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Dosage:25 mg/kg; 50 mg/kg
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Administration:p.o.; daily; 14 days
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Result:Significantly inhibited LS174T xenograft tumor growth relative to vehicle control.
Did not cause significant body weight loss.
Exhibited a more pronounced inhibitory effect at 50 mg/kg than at 25 mg/kg.
Significantly reduced tumor weights in both treatment groups compared to vehicle control.\nSignificantly inhibited HCT116 xenograft tumor growth relative to vehicle control.
Did not cause significant body weight loss.
Significantly reduced tumor weights in both treatment groups compared to vehicle control.
Chemical Information
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Peso molecular 368.36
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Fòrmula C20H15F3N4
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SMILES
FC(F)(F)C1=CC=C(C2=NN3C(NCC[C@@H]3C4=CC=CC=C4)=C2C#N)C=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 357 Related Classifications
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