Pipendoxifene - CAS 198480-55-6

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.

Estrogen Receptor/ERR, Others

Endocrinology/Hormones, Others

198419

C29H32N2O3

456.58

C(N1C(=C(C)C=2C1=CC=C(O)C2)C3=CC=C(O)C=C3)C4=CC=C(OCCN5CCCCC5)C=C4

-20°C

Ice Packs

Small Compound