1. Vitamin D Related/Nuclear Receptor Apoptosis
  2. Estrogen Receptor/ERR Caspase
  3. Ospemifene

Ospemifene (FC-1271a) is an orally active and non-estrogenic selective estrogen receptor modulator (SERM) with Ki values of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene inhibits caspase-3 activity. Ospemifene inhibits neuronal degeneration, prevents bone loss, and increases vaginal weight and vaginal epithelial height. Ospemifene has anticancer activity against breast cancer.

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Ospemifene Chemical Structure

Ospemifene Chemical Structure

CAS No. : 128607-22-7

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Ospemifene:

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  • Biological Activity

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Description

Ospemifene (FC-1271a) is an orally active and non-estrogenic selective estrogen receptor modulator (SERM) with Ki values of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene inhibits caspase-3 activity. Ospemifene inhibits neuronal degeneration, prevents bone loss, and increases vaginal weight and vaginal epithelial height. Ospemifene has anticancer activity against breast cancer[1][2][3][4][5][6].

IC50 & Target[5]

Caspase-3

 

Cellular Effect
Cell Line Type Value Description References
MCF7 IC50
> 100 μM
Compound: 1
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 25164760]
MCF7 IC50
> 50 μM
Compound: Ospemifene
Cytotoxicity against human ER-positive MCF7 cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against human ER-positive MCF7 cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 26972118]
MCF7 IC50
55 μM
Compound: 1
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 96 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 96 hrs by MTT assay
[PMID: 25164760]
MDA-MB-231 IC50
> 100 μM
Compound: 1
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 25164760]
MDA-MB-231 IC50
> 100 μM
Compound: 1
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 96 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 96 hrs by MTT assay
[PMID: 25164760]
MDA-MB-231 IC50
> 50 μM
Compound: Ospemifene
Cytotoxicity against human ER-negative MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against human ER-negative MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay
[PMID: 26972118]
In Vitro

Ospemifene (100 pM-30 μM) binds with essentially comparable affinity to the ER-α and ER-β isoforms and effectively antagonize ERE-mediated transactivation in MCF-7 cells[1].
Ospemifene (0.1 nM-10 μM) does not significantly promote the growth of MCF-7 cells[3].
Ospemifene (0.1-10 μM; 4-6 days) inhibits the growth of MCF-7 cells and has no significant effect on the growth of MDA-MB-231 cells[4].
Ospemifene (0.1-10 μM; posttreatment) decreases hypoxia- and ischemia- induced LDH release, caspase-3 activity, neuronal cell degeneration in primary neocortical cell cultures subjected to hypoxia and/or ischemia[5].

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

Cell Proliferation Assay[4]

Cell Line: MCF-7
Concentration: 0.1 μM, 1.0 μM, 5.0 μM, 10.0 μM
Incubation Time: 4-6 days
Result: Inhibited the growth of MCF-7 cells.
Increased its growth inhibitory effect as its concentration increases.
Had a cell growth rate of 95.4% of the control at 0.1 μM and 56.4% of the control at 10.0 μM.
In Vivo

Ospemifene (10-100 mg/kg/day; p.o.; once daily; 14-28 days) increases vaginal weight and has a greater effect on increasing vaginal epithelial height compared with Raloxifene (HY-13738) in ovariectomized rats[1].
Ospemifene (1-10 mg/kg; p.o.; 4 weeks) can prevent bone loss, maintain the trabecular bone volume of the distal femur, prevent the decrease of bone strength in ovariectomized rats[3].
Ospemifene (10-100 mg/kg; p.o.; once daily; 7 days) inhibits the growth of MCF-7 tumors in the athymic, ovariectomized mouse model with MCF-7 human tumor xenografts[4].
Ospemifene (5-50 mg/kg; p.o.; daily) effectively prevents breast cancer in the MTag.Tg transgenic mouse model[6].

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

Animal Model: Animal Model: Adult female Sprague Dawley rats (weight about 300 g at the beginning of the experiments, 2.5 months old), ovariectomized model[3]
Dosage: 0.1 mg/kg, 1 mg/kg, 10 mg/kg
Administration: Orally, once daily, 4 weeks
Result: Prevented bone loss by maintaining the trabecular bone volume of the distal femur and preventing the loss of bone strength at doses of 1 and 10 mg/kg.
Prevented the OVX-induced increase in serum cholesterol in a dose-dependent manner.
Had no significant effect on uterine wet weight or morphology at 0.1 or 1 mg/kg.
Had a slightly estrogenic effect at 10 mg/kg.
Animal Model: Female Sprague Dawley rats, DMBA (HY-W011845)-induced breast carcinoma model[3]
Dosage: 10 mg/kg, 50 mg/kg
Administration: Orally, 4 weeks
Result: Reduced the number of breast tumors.
Reduced the number of growing tumors, increased the number of dormant or regressing tumors, and even caused some tumors to disappear.
Animal Model: Female athymic nude mice (8-12 weeks old; nu/nu-BALB/cABom), MCF-7 cell-transplanted tumor model after OVX and estrogen supplementation[3]
Dosage: 1 mg/kg, 10 mg/kg, 50 mg/kg
Administration: Oral gavage (p.o.), 48 days
Result: Cannot sustain tumor growth in the absence of estrogen.
Had no effect at 1 mg/kg and resulted in slower tumor regression at 10 or 50 mg/kg.
Clinical Trial
Molecular Weight

378.89

Formula

C24H23ClO2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClCC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCO)C=C2)\C3=CC=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (263.93 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6393 mL 13.1964 mL 26.3929 mL
5 mM 0.5279 mL 2.6393 mL 5.2786 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.60 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.60 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6393 mL 13.1964 mL 26.3929 mL 65.9822 mL
5 mM 0.5279 mL 2.6393 mL 5.2786 mL 13.1964 mL
10 mM 0.2639 mL 1.3196 mL 2.6393 mL 6.5982 mL
15 mM 0.1760 mL 0.8798 mL 1.7595 mL 4.3988 mL
20 mM 0.1320 mL 0.6598 mL 1.3196 mL 3.2991 mL
25 mM 0.1056 mL 0.5279 mL 1.0557 mL 2.6393 mL
30 mM 0.0880 mL 0.4399 mL 0.8798 mL 2.1994 mL
40 mM 0.0660 mL 0.3299 mL 0.6598 mL 1.6496 mL
50 mM 0.0528 mL 0.2639 mL 0.5279 mL 1.3196 mL
60 mM 0.0440 mL 0.2199 mL 0.4399 mL 1.0997 mL
80 mM 0.0330 mL 0.1650 mL 0.3299 mL 0.8248 mL
100 mM 0.0264 mL 0.1320 mL 0.2639 mL 0.6598 mL
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  • 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.

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