Ratutrelvir
Ratutrelvir is a NF-κB p65 inhibitor. Ratutrelvir blocks the translocation of NF-κB p65 from the cytoplasm to the nucleus, reduces the phosphorylation levels of NF-κB p65 and IκBα, and inhibits the DNA-binding activity of NF-κB p65. Ratutrelvir inhibits the migration and invasion abilities of breast cancer cells, and reduces their viability and colony-forming capacity. Ratutrelvir can be used for the research of luminal A breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 2929236-94-0
- Formula: C27H32F3N5O4
- Molecular Weight:547.57
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Ratutrelvir (0-100 μM; 24-96 h) potently reduces the viability of MCF-7 cells, with an IC50 of 53.9 μM; it only exerts weak inhibitory effects on MDA-MB-231 and MCF-10A cells at high concentrations, and shows no inhibitory effect on the viability of BT474 cells[1].
Ratutrelvir (0-100 μM; 48 h) inhibits colony formation of MCF-7 cells in a concentration-dependent manner, suppresses colony formation of MDA-MB-231 cells at a concentration of 50 μM, and exerts no effect on colony formation of BT474 cells[1].
Ratutrelvir (25 μM; 48 h) significantly inhibits the migration of MCF-7 cells, but exerts no effect on the migration of MDA-MB-231 or BT474 cells[1].
Ratutrelvir (12.5 μM; 72 h) significantly reduces the invasive ability of MCF-7 cells, but exerts no effect on the invasive ability of MDA-MB-231 or BT474 cells[1].
Ratutrelvir (0-100 μM; 12 h) inhibits the NF-κB pathway in MCF-7 cells by reducing the levels of p-NF-κB p65 and p-IκBα and blocking the nuclear translocation of NF-κB p65, but exerts no effect on the NF-κB pathway in MDA-MB-231 or BT474 cells[1].
Ratutrelvir (50 μM; 2, 4, 6, 8, 12 h) inhibits the DNA-binding activity of NF-κB in MCF-7 cells in a time-dependent manner in vitro, but exerts no effect on this activity in MDA-MB-231 or BT474 cells[1].
Ratutrelvir (0-100 μM; 96 h) inhibits TNF-α-mediated NF-κB activation in MCF-7 cells, and TNF-α can partially reverse the inhibitory effects of Ratutrelvir on the proliferation, migration and invasion of MCF-7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human MCF-7, MDA-MB-231, BT474, and MCF-10A breast cells
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Concentration:0, 12.5, 25, 50, 75, 100 μM
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Incubation Time:24, 48, 96 h
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Result:Reduced MCF-7 cell viability in a concentration- and time-dependent manner, with an IC50 of 53.9 μM.
Showed a slight inhibitory effect on MDA-MB-231 cells at 75 μM.
Showed no inhibitory effect on BT474 cells at up to 100 μM.
Inhibited MCF-10A cell proliferation only at 75 μM, and this effect was significantly weaker than that on MCF-7 cells.
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Cell Line:Human MCF-7, MDA-MB-231, and BT474 breast cancer cells
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Concentration:0, 12.5, 25, 50, 75, 100 μM
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Incubation Time:48 h
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Result:Reduced the percentage of surviving MCF-7 cell colonies in a concentration-dependent manner.
Reduced MDA-MB-231 colony formation at 50 μM.
Showed no effect on BT474 colony formation.
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Cell Line:Human MCF-7, MDA-MB-231, and BT474 breast cancer cells
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Concentration:25 μM
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Incubation Time:48 h
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Result:Significantly inhibited the migration of MCF-7 cells.
Did not suppress the migration of MDA-MB-231 or BT474 cells.
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Cell Line:Human MCF-7, MDA-MB-231, and BT474 breast cancer cells
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Concentration:12.5 μM
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Incubation Time:72 h
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Result:Significantly reduced the invasiveness of MCF-7 cells.
Did not significantly affect the invasiveness of MDA-MB-231 or BT474 cells.
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Cell Line:Human MCF-7, MDA-MB-231, and BT474 breast cancer cells
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Concentration:0, 25, 50, 75,100 μM (whole-cell lysates); 50 μM (nuclear/cytoplasmic fractionation)
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Incubation Time:12 h
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Result:Decreased the expression of p-NF-κB p65 and p-IκBα in a concentration-dependent manner in MCF-7 cells, while NF-κB p65 and IκBα protein levels were not markedly altered.
Notably suppressed the nuclear localization of NF-κB p65 in MCF-7 cells.
Did not alter the levels of p-NF-κB p65, p-IκBα, NF-κB p65, or IκBα in MDA-MB-231 and BT474 cells.
Chemical Information
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CAS No. 2929236-94-0
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Molecular Weight 547.57
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Formula C27H32F3N5O4
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SMILES
CC1(C)[C@](CN2C([C@H](C(C)(C)C)NC(C(F)(F)F)=O)=O)([H])[C@@]1([H])[C@H]2C(N[C@@H](CC3C(NC4=CC=CC=C43)=O)C#N)=O
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Synonyms
TRX01
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)