2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. Antiestrogenic agent-1

Antiestrogenic agent-1, an organophosphorus 13α-estrone derivative, is an antiestrogenic agent. Antiestrogenic agent-1 can disrupt estrogen signaling by inhibiting estrogen-mediated transcriptional activity. Antiestrogenic agent-1 can inhibit cancer cells proliferation, migration, invasion and induce G1-phase arrest. Antiestrogenic agent-1 mitigates estrogen-induced uterine growth in immature rats and inhibits tumor growth in a murine triple-negative breast cancer mice model. Antiestrogenic agent-1 can be used for the researches of cancer and endocrinology,such as breast cancer, oropharyngeal squamous cell carcinoma.

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

Antiestrogenic agent-1

Antiestrogenic agent-1 Chemical Structure

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Antiestrogenic agent-1 Related Antibodies

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Description

Antiestrogenic agent-1, an organophosphorus 13α-estrone derivative, is an antiestrogenic agent. Antiestrogenic agent-1 can disrupt estrogen signaling by inhibiting estrogen-mediated transcriptional activity. Antiestrogenic agent-1 can inhibit cancer cells proliferation, migration, invasion and induce G1-phase arrest. Antiestrogenic agent-1 mitigates estrogen-induced uterine growth in immature rats and inhibits tumor growth in a murine triple-negative breast cancer mice model. Antiestrogenic agent-1 can be used for the researches of cancer and endocrinology,such as breast cancer, oropharyngeal squamous cell carcinoma[1].

In Vitro

Antiestrogenic agent-1 (Compound EDPO) (0.4-60 μM; 24 h) inhibits estrogen-mediated transcriptional activity in T47D-KBluc cells with an IC50 of 10 μM[1].
Antiestrogenic agent-1 shows substantial
antiproliferative effect against T47D breast cancer cells and UPCI-SCC-131 oropharyngeal squamous cell carcinoma cells, with IC50 values of 7.2 μM and 5.3 μM[1].
Antiestrogenic agent-1 (1.75-7 μM; 12-72 h) induces time- and dose-dependent G1-phase cell cycle arrest in T47D cells[1].
Antiestrogenic agent-1 (2.5-5 μM (UPCI-SCC-131); 3.5-7 μM (T47D); 24-48 h) reduces migration of UPCI-SCC-131 and T47D cells in a time- and concentration-dependent manner[1].
Antiestrogenic agent-1 (3.5-7 μM; 48 h) decreases the invasive capacity of T47D cells[1].

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

Antiestrogenic agent-1 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: T47D (ERα+ human breast cancer cell line)
Concentration: 1.75, 3.5 and 7 μM
Incubation Time: 12, 24, 48, 72 h
Result: Induced substantial time- and dose-dependent G1-phase cell cycle arrest.
Increased G1 population and decreased S phase population at all time intervals, showed most pronounced arrest at 24 h.

Cell Migration Assay [1]

Cell Line: UPCI-SCC-131 (human oropharyngeal squamous cell carcinoma cell line), T47D (ERα+ human breast cancer cell line)
Concentration: 2.5 and 5 μM (UPCI-SCC-131); 3.5 and 7 μM (T47D)
Incubation Time: 24, 48 h (UPCI-SCC-131); 24, 48 h (T47D)
Result: Significantly reduced cell migration in both cell lines in a time- and concentration-dependent manner.
Achieved significant effect at both concentrations at 24 h, and only at 5 μM at 48 h for UPCI-SCC-131.
Achieved significant effect at both concentrations at 24 and 48 h for T47D.
In Vivo

Antiestrogenic agent-1 (Compound EDPO) (60-600 μg/g; s.c.; daily; 3 days) effectively inhibits estrogen receptor alpha-mediated uterine tissue growth in 21-day-old female immature SD rats[1].
Antiestrogenic agent-1 (10-30 μg/g; i.p.; daily; 16 days) exerts significant dose-dependent antitumor activity against BALB/c mice with 4T1 triple-negative breast cancer[1].

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

Animal Model: Sprague-Dawley (female, 21 days old, 35-47 g, 17β-estradiol-induced uterine growth)[1]
Dosage: 60, 600 μg/g
Administration: S.c.; daily; 3 days
Result: Mitigated 17β-estradiol-induced uterine growth in a dose-dependent manner.
Showed no significant difference in inhibitory effects on uterine tissue growth compared to Fulvestrant (HY-13636) at the higher dose.
Animal Model: BALB/c mice (female, 8-10 weeks old, orthotopic 4T1 murine breast cancer)[1]
Dosage: 10, 30 μg/g
Administration: I.p.; daily; 16 days
Result: Induced a significant and dose-dependent reduction in tumor growth throughout the 16-day treatment period.
Reduced tumor growth significantly from day 2 onwards at the higher dose.
Molecular Weight

498.59

Formula

C32H35O3P
SMILES

C[C@@]1([C@](C[C@H]2CP(C3=CC=CC=C3)(C4=CC=CC=C4)=O)([H])[C@]5([H])CCC6=C(C=CC(OC)=C6)[C@@]5([H])CC1)C2=O
Shipping

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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Antiestrogenic agent-1 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:

Antiestrogenic agent-1Antiestrogenic agent1Antiestrogenic agent 1Estrogen Receptor/ERRERαoropharyngeal carcinoma cellsmurine triple-negative breast cancerT47D-KBlucUPCI-SCC-131T47D4T1Inhibitorinhibitorinhibit

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