| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
Pipendoxifene targets estrogen receptor alpha (ERα) as a selective estrogen receptor modulator (SERM). It antagonizes the binding of estradiol to ERα, thereby inhibiting ERα-mediated gene expression and interfering with estrogen activity. The compound acts as an agonist or antagonist depending on the target tissue. It inhibits estrogen-stimulated growth in ER-alpha-positive human breast cancer cells and possesses intrinsic estrogenic activity depending on tissue type.
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| ln Vitro |
Pipendoxifene possesses exceptional preclinical pharmacology profiles, making it a novel 2-phenylindole selective estrogen receptor modulator (SERM) that has been chosen for additional research in the treatment of metastatic breast cancer [1].
In ER-alpha-positive human MCF-7 breast carcinoma cells, ERA-923 inhibits estrogen-stimulated growth with an IC50 of 0.2 nM, associated with cytostasis. It inhibits estrogen binding to ER-alpha with an IC50 of 14 nM. A MCF-7 variant with inherent resistance to tamoxifen (10-fold) or 4-OH tamoxifen (>1000-fold) retains complete sensitivity to ERA-923. In preclinical models, ERA-923 has improved efficacy and safety compared with tamoxifen. In combination with temsirolimus, it showed excellent anticancer activity. |
| ln Vivo |
Pipendoxifene demonstrates exceptional preclinical pharmacology profiles and has been selected for further development as a treatment for metastatic breast cancer. In preclinical models, ERA-923 has improved efficacy and safety compared with tamoxifen. In combination with temsirolimus, ERA-923 showed excellent anticancer activity in preclinical models. The compound inhibits estrogen-stimulated growth by inhibiting cell growth and has potent and selective estrogen-regulating effects with few uterine side effects.
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| Enzyme Assay |
Specific cell-free enzyme/receptor binding assay protocols for Pipendoxifene involve competitive binding assays to determine inhibition of estrogen binding to ER-alpha, with an IC50 of 14 nM. Radioligand displacement assays using tritiated estradiol and recombinant ER-alpha protein are typically employed to assess binding affinity. The compound’s selectivity for ER-alpha over other nuclear receptors can be evaluated using panel screening assays.
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| Cell Assay |
In vitro cell-based assays for Pipendoxifene use ER-alpha-positive human MCF-7 breast carcinoma cells. Cells are treated with ERA-923 at varying concentrations, and estrogen-stimulated growth inhibition is assessed to determine IC50 values (0.2 nM). Tamoxifen-resistant MCF-7 variants are used to evaluate retained sensitivity. Cell proliferation is measured using standard assays such as MTT or BrdU incorporation, and cytostasis is confirmed through cell cycle analysis.
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| Animal Protocol |
In vivo animal studies for Pipendoxifene are not extensively detailed in the available literature. Preclinical models have been used to evaluate ERA-923’s efficacy and safety compared with tamoxifen. Combination studies with temsirolimus have shown excellent anticancer activity in preclinical models. Typical in vivo evaluation would involve xenograft mouse models bearing estrogen-dependent breast tumors, with treatment administered orally and tumor growth inhibition monitored.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic properties of Pipendoxifene are not extensively reported. The compound has a molecular formula of C29H32N2O3, a molecular weight of 456.58 g/mol, and a LogP of 5.878. It appears as an off-white to light yellow solid powder. The compound has a boiling point of 685.8°C at 760 mmHg and a flash point of 368.6°C. It contains two hydrogen bond donors and four hydrogen bond acceptors, with seven rotatable bonds. The compound is soluble in DMSO.
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| Toxicity/Toxicokinetics |
Specific toxicological data for Pipendoxifene are not detailed in the available literature. The compound is classified for research use only and is not intended for human therapeutic use. In preclinical models, ERA-923 has demonstrated improved safety compared with tamoxifen. It has been shown to have potent and selective estrogen-regulating effects with few uterine side effects. Standard toxicology studies would be expected for a compound selected for development as a breast cancer treatment.
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| References | |
| Additional Infomation |
ERA-923 (piperidoxifene), an estrogen receptor modulator, is being evaluated for the treatment of breast cancer. Piperidoxifene is a novel 2-phenylindole selective estrogen receptor modulator (SERM) with excellent preclinical pharmacological properties and has been selected for further development in the treatment of metastatic breast cancer. Piperidoxifene is a nonsteroidal 2-phenylindole selective estrogen receptor modulator (SERM) with potential antitumor activity. Piperidoxifene antagonizes the binding of estradiol to estrogen receptor α (ERα), thereby inhibiting ERα-mediated gene expression, interfering with estrogen activity, and inhibiting estrogen-stimulated growth in estrogen-dependent breast cancer. Furthermore, the drug also possesses intrinsic estrogenic activity, depending on tissue type. Drug Indications It has been studied for the treatment of breast cancer. Mechanism of Action ERA-923 inhibits estrogen-stimulated growth by inhibiting cell growth. It has been shown to have a potent and selective estrogen-regulating effect with few uterine side effects.
Pipendoxifene (ERA-923) (CAS 198480-55-6) is a novel 2-phenylindole selective estrogen receptor modulator (SERM) selected for further development as a treatment for metastatic breast cancer. It potently inhibits estrogen binding to ER-alpha with an IC50 of 14 nM and inhibits estrogen-stimulated growth in MCF-7 cells with an IC50 of 0.2 nM. The compound has been evaluated for breast cancer treatment and has demonstrated improved efficacy and safety compared with tamoxifen in preclinical models. No active clinical trial data are available in the provided sources. |
| Molecular Formula |
C29H32N2O3
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|---|---|
| Molecular Weight |
456.58
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| Exact Mass |
456.241
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| CAS # |
198480-55-6
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| Related CAS # |
Pipendoxifene hydrochloride;245124-69-0
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| PubChem CID |
6433099
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.2g/cm3
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| Boiling Point |
685.8ºC at 760mmHg
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| Flash Point |
368.6ºC
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| Vapour Pressure |
1.93E-19mmHg at 25°C
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| Index of Refraction |
1.628
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| LogP |
5.878
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
34
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| Complexity |
611
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JICOGKJOQXTAIP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H32N2O3/c1-21-27-19-25(33)11-14-28(27)31(29(21)23-7-9-24(32)10-8-23)20-22-5-12-26(13-6-22)34-18-17-30-15-3-2-4-16-30/h5-14,19,32-33H,2-4,15-18,20H2,1H3
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| Chemical Name |
2-(4-hydroxyphenyl)-3-methyl-1-[[4-(2-piperidin-1-ylethoxy)phenyl]methyl]indol-5-ol
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| Synonyms |
ERA-923 ERA 923 ERA923
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1902 mL | 10.9510 mL | 21.9020 mL | |
| 5 mM | 0.4380 mL | 2.1902 mL | 4.3804 mL | |
| 10 mM | 0.2190 mL | 1.0951 mL | 2.1902 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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