VPC-16606
VPC-16606 is a selective inhibitor targeting the activation function 2 (AF2) domain of estrogen receptor α (ERα). VPC-16606 blocks the interaction between ERα and coactivators, inhibits the activity of both wild-type and clinically drug-resistant mutant ERα, and exerts inhibitory effects on hormone-resistant breast cancer cells. VPC-16606 can be used in breast cancer research.
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- CAS No.: 2027540-49-2
- Formule: C17H13ClN2O2S
- Masse moléculaire:344.81
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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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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
VPC-16606 (24 h) potently inhibits the transcriptional activity of ERα in T47D-KBluc human breast cancer cells, with an IC50 of 0.31 μM[1].
VPC-16606 (1.6-50 μM; 24 h) blocks the interaction between ERα and the coactivator SRC-3 in MDA-MB-231 cells[1].
VPC-16606 (0-50 μM; 96 h) exerts ERα-specific antiproliferative effects on ERα-positive, Tamoxifen (HY-13757A)-resistant human breast cancer cells[1].
VPC-16606 (0.38-6 μM; 24 h) downregulates ERα-dependent gene expression in MCF7 cells and Tamoxifen (HY-13757A)-resistant TamR3 human breast cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:ERα-positive (MCF7, T47D, TamR3) human breast cancer cells; ERα-negative MDA-MB-231 cells
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Concentration:Up to 50 μM (2-fold dilution range)
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Incubation Time:96 h
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Result:Significantly reduced the growth of ERα-positive MCF7, T47D, and Tamoxifen-resistant TamR3 cells in a dose-dependent manner, with no effect on ERα-negative MDA-MB-231 cells.
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Cell Line:MCF7 and TamR3 human breast cancer cells
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Concentration:0.38, 0.75, 1.5, 3, 6 μM
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Incubation Time:24 h
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Result:Significantly down-regulated the mRNA expression of ERα target genes pS2, PR, Cyclin D1, and CDC2 in both MCF7 and TamR3 cells at all tested concentrations.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rag2 (female, 10-12 weeks old, intraperitoneal implantation of luciferase-modified MCF7LUC ERα-positive human breast cancer cells, pre-implantation 60-day release estradiol pellet supplementation)[1]
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Dosage:51 mg
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Administration:i.p. (via implanted Alzet pump); continuous
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Result:Reduced total light emission from tumors at 60 days post-cell injection compared to vehicle-treated controls.
Reduced tumor burden compared to vehicle-treated controls.
Achieved median survival time of 60 days, with 100% survival to study termination at day 61.
Chemical Information
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CAS No. 2027540-49-2
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Masse moléculaire 344.81
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Formule C17H13ClN2O2S
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SMILES
O=C1C(=NN(C(=O)C)C=2C=CC=CC2Cl)SC=3C1=CC=CC3C
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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)
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