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Compound Overview
Pipendoxifene (CAS 198480-55-6) is a research-grade small molecule supplied by TargetMol.
Physical Properties
| CAS Number | 198480-55-6 |
|---|---|
| Molecular Formula | C29H32N2O3 |
| Molecular Weight | 456.58 g/mol |
| SMILES | C(N1C(=C(C)C=2C1=CC=C(O)C2)C3=CC=C(O)C=C3)C4=CC=C(OCCN5CCCCC5)C=C4 |
| Form | Solid |
| Shipping | Room Temperature (RT) |
Biological Activity
Pipendoxifene, also known as ERA-923, is a new antiestrogen with potential anticancer activity. ERA-923 potently inhibits estrogen binding to ER-alpha (IC50 = 14 nM). In ER-alpha-positive human MCF-7 breast carcinoma cells, ERA-923 inhibits estrogen-stimulated growth (IC50 = 0.2 nM) associated with cytostasis. In vitro, 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 an improved efficacy and safety compared with tamoxifen. In the combination with temsirolimus, ERA-923 showed excellent anticancer activity in preclinical models.
Safety & Regulatory
For Research Use Only (RUO). Not for therapeutic, diagnostic, or clinical use. Wear appropriate PPE and consult the Safety Data Sheet (SDS) prior to handling.
Sonication time depends on compound solubility and concentration. In most cases, 1–3 minutes of intermittent bath sonication is sufficient to dissolve small molecule compounds in DMSO. For poorly soluble compounds, warming the solvent to 37–50 °C combined with brief vortexing between sonication pulses can improve dissolution. If the compound remains undissolved, prepare a more dilute stock solution.
PEG300 has moderate viscosity, which facilitates the dissolution and administration of drugs, while also providing good tolerability without adverse effects on animals. PEG400 can replace PEG300. PEG600 is not very recommended because its melting point is close to room temperature.
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- Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
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