2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. 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.

For research use only. We do not sell to patients.

VPC-16606

VPC-16606 Chemical Structure

CAS No. : 2027540-49-2

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VPC-16606 Related Antibodies

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Description

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[1].

In Vitro

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.

VPC-16606 Related Antibodies

Cell Viability Assay[1]

Cell Line: ERα-positive (MCF7, T47D, TamR3) human breast cancer cells; ERα-negative MDA-MB-231 cells
Concentration: Up to 50 μM (2-fold dilution range)
Incubation Time: 96 h
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.

Real Time qPCR[1]

Cell Line: MCF7 and TamR3 human breast cancer cells
Concentration: 0.38, 0.75, 1.5, 3, 6 μM
Incubation Time: 24 h
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.
In Vivo

VPC-16606 (51 mg; i.p.) reduces intraperitoneal breast cancer tumor burden in female Rag2 mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: 51 mg
Administration: i.p. (via implanted Alzet pump); continuous
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.
Molecular Weight

344.81

Formula

C17H13ClN2O2S
CAS No.
SMILES

O=C1C(=NN(C(=O)C)C=2C=CC=CC2Cl)SC=3C1=CC=CC3C
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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VPC-16606 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VPC-166062027540-49-2VPC16606VPC 16606Estrogen Receptor/ERRestrogen receptortamoxifen-resistant cellsERαAF2 siteMCF7 human breast cancer cellsRag2 miceT47D-KBluc human breast cancer cellsMDA-MB-231 cellsInhibitorinhibitorinhibit

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