Anticancer agent-367
Anticancer agent-367 is a 3-hydroxy-3′,4′,5′-trimethoxyflavone derivative with selective cytotoxicity against osteosarcoma cells (IC50 = 14 μM). Anticancer agent-367 reduces AKT phosphorylation levels in 143B osteosarcoma cells and downregulates the expression of epithelial-mesenchymal transition-related genes such as ZEB1, MMP2, and MMP9. The combination of Anticancer agent-367 with Doxorubicin (HY-15142A) produces a synergistic antiproliferative effect on 143B cells. Anticancer agent-367 can be used in osteosarcoma-related research.
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- Formule: C23H25NO6
- Masse moléculaire:411.45
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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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Activité biologique
Description
IC50 & Target
[1]|
Akt |
MMP-9 |
MMP-2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 143B | IC50 |
14 μM
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Cytotoxicity against human 143B osteosarcoma cells assessed as viability reduction after 48 hrs by WST-8/CCK-8 assay.
Cytotoxicity against human 143B osteosarcoma cells assessed as viability reduction after 48 hrs by WST-8/CCK-8 assay.
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42664600 |
| 143B | IC50 |
2.0 μM
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Antiproliferative activity against human 143B osteosarcoma cells assessed as growth inhibition after 48 hrs by SRB assay.
Antiproliferative activity against human 143B osteosarcoma cells assessed as growth inhibition after 48 hrs by SRB assay.
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42664600 |
In Vitro
Anticancer agent-367 (compound 6A) (0-160 μmol/L) inhibits 143B osteosarcoma cell viability and growth, with a WST-8 IC50 of 14 μmol/L and an SRB IC50 of 2.0 μmol/L; it exhibits low toxicity toward MRC-5 lung fibroblasts[1].
Anticancer agent-367 (0-56 μmol/L) produced a synergistic effect with doxorubicin in 143B osteosarcoma cells, with CI = 0.9272 and DRI >1, supporting a reduction in the doxorubicin dose[1].
Anticancer agent-367 (7-14 μmol/L; 48 h) reduces p-AKT in 143B osteosarcoma cells at 14 μmol/L alone or in combination with doxorubicin[1].
Anticancer agent-367 (7-14 μmol/L; 48 h) downregulates the EMT-related genes ZEB1, MMP2, and MMP9 in 143B osteosarcoma cells, and further downregulates MMP9[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:143B human osteosarcoma cells, MRC-5 human fetal lung fibroblasts
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Concentration:0, 10, 20, 40, 80, 160 μmol/L
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Incubation Time:48 h
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Result:Produced dose-dependent inhibition of 143B cell viability and growth.
Showed low toxicity toward MRC-5 cells.
At 80 μmol/L, resulted in 5% inhibition of cell viability.
Displayed lower cytotoxicity than 6b at higher concentrations (>80 μmol/L).
Below 40 μmol/L, did not reduce MRC-5 cell viability.
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Cell Line:143B human osteosarcoma cells
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Concentration:7 and 14 μmol/L
0.075 and 0.15 μmol/L Doxorubicin -
Incubation Time:48 h
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Result:Reduced p‑AKT levels showed no significant change when compound 6a was applied as a single agent at 7 μmol/L.
Reduced p‑AKT levels significantly when 7 μmol/L compound 6a was combined with Doxorubicin.
Reduced p‑AKT expression markedly at 14 μmol/L regardless of monotherapy or Doxorubicin combination, which indicated the inhibition of AKT signaling.
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Cell Line:143B human osteosarcoma cells
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Concentration:7 and 14 μmol/L
0.075 and 0.15 μmol/L Doxorubicin -
Incubation Time:48 h
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Result:Downregulated ZEB1, MMP2, and MMP9 in a concentration‑dependent manner when used as a single agent.
Exhibited similar down‑regulation trends for MMP2 and MMP9 expression under combination with doxorubicin, yet produced no significant influence on ZEB1 levels.
Exerted additional suppressive effect on MMP9 expression.
Chemical Information
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Masse moléculaire 411.45
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Formule C23H25NO6
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SMILES
O=C1C2=CC=C(N3CCCCC3)C=C2OC(C4=CC(OC)=C(OC)C(OC)=C4)=C1O
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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-367 Related Classifications
HY-189737 Related Classifications
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