ER degrader 5
ER degrader 5 is a potent estrogen receptor (ER) degrader. ER degrader 5 shows anti-proliferation activity. ER degrader 5 can be used for the research of breast cancer.
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- CAS. Nr.: 2913192-47-7
- Formel: C26H18F2O4S
- Molecular Weight:464.48
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
0.055 μM
Compound: 27b
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Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 5 days by MTT assay
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 5 days by MTT assay
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[PMID: 37019030] |
In Vitro
ER degrader 5 (compound 27d) (5 days) inhibits the proliferation of MCF-7 cells, with an IC50 of 55 nM[1].
ER degrader 5 blocks the cell cycle at the G0/G1 phase in MCF-7 cells[1].
ER degrader 5 (1 nM-10 μM; 24 h) degrades estrogen receptor (ER) in MCF-7 cells[1].
ER degrader 5 (1-10 μM; 24 h) drastically decreases the expression levels of GREB1, PGR, and TFF1 in 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:MCF-7 cells
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Concentration:1, 10, 100, 1000, 10000 nM
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Incubation Time:24 hours
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Result:Degraded ER in a dose-dependent manner.
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Cell Line:MCF-7 cells
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Concentration:1, 5, 10 μM
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Incubation Time:24 hours
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Result:Decreased the expression levels of GREB1, PGR, and TFF1 in a dose-dependent manner.
In Vivo
ER degrader 5 (3 mg/kg; i.v.) exhibits half-life of 1.23 h, Cmax of 4497 ng/mL[1].
ER degrader 5 (30 mg/kg; p.o.) produces an oral bioavailability of 62.9%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nude mice injected with MCF-7 cells[1]
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Dosage:30 mg/kg
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Administration:I.p. daily for 30 days
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Result:Inhibited tumor growth and observed no significant body weight loss.
Chemical Information
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CAS. Nr. 2913192-47-7
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Molecular Weight 464.48
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Formel C26H18F2O4S
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SMILES
O=C(C1=C(C=C(C=C1C)F)C)C(SC2=CC(F)=CC=C23)=C3OC4=CC=C(C=C4)/C=C/C(O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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