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Endoxifen, (Z)-

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Axon 2221 CAS [112093-28-4] MF C25H27NO2MW 373.49 Purity: 99% Soluble in 0.1N HCl(aq) and DMSO Description The more active (Z)-isomer of (E/Z)-Endoxifen (Axon 2190), an active metabolite of Tamoxifen and a selective estrogen receptor modulator (SERM; IC50 value 0.01–0.10 μM in estrogen-stimulated proliferation assay in MCF-7 cells); Potently inhibits the growth of estrogen-stimulated BT474 cells. Approximately 100-fold more potent as an antagonist of the ERα than the parent drug. Z-Endoxifen may provide a new and better treatment for women with estrogen receptor (ER) positive breast cancer. References Certificates Categories Extra info P. Elkins et al. Characterization of the isomeric configuration and impurities of (Z)-endoxifen by 2D-NMR, high resolution LC-MS, and quantitative HPLC analysis. J. Pharm. Biomed. Anal. 2014, 88, 174-179. J.R. Hawse et al. Endoxifen’s Molecular Mechanisms of Action Are Concentration Dependent and Different than That of Other Anti-Estrogens. PLoS One. 2013, 8, e54613. A Ahmad et al. Endoxifen, a New Cornerstone of Breast Cancer Therapy: Demonstration of Safety, Tolerability, and Systemic Bioavailability in Healthy Human Subjects. Clin. Pharmacol. Ther. 2010, 88(6), 814–817. M.D. Johnson et al. Pharmacological Characterization of 4-hydroxy-N-desmethyl Tamoxifen, a Novel Active Metabolite of Tamoxifen. Breast Cancer Research and Treatment 2004, 85, 151-159. Certificate of Analysis Material Safety Data Sheet Cell Signaling & Oncology Endocrinology Estrogen (ER) NR3A The more active (Z)-isomer of Endoxifen (SERM; Axon 2190) Chemical name (Z)-4-(1-(4-(2-(methylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenol Parent CAS No. [112093-28-4] Order Size Unit Price Stock 5 mg €155.00 In Stock

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Endoxifen, (Z)-

Based on 14 reference(s) in Google Scholar 8 10 14

Axon 2221

CAS [112093-28-4]

MF C25H27NO2
MW 373.49

Purity: 99%
Soluble in 0.1N HCl(aq) and DMSO

Endoxifen, (Z)-

Description

The more active (Z)-isomer of (E/Z)-Endoxifen (Axon 2190), an active metabolite of Tamoxifen and a selective estrogen receptor modulator (SERM; IC50 value 0.01–0.10 μM in estrogen-stimulated proliferation assay in MCF-7 cells); Potently inhibits the growth of estrogen-stimulated BT474 cells.
Approximately 100-fold more potent as an antagonist of the ERα than the parent drug. Z-Endoxifen may provide a new and better treatment for women with estrogen receptor (ER) positive breast cancer.