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Description: Endoxifen HCl, an active metabolite of Tamoxifen, is a potent and selective estrogen receptor antagonist and has been found to be effective in patients that have failed previous hormonal therapies. Endoxifen shows anti-estrogenic effects, and decreases the E2-induced PR expression in MCF-7 cells. Endoxifen also blocks ER-alpha transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation. In MCF7, HS 578T, and BT-549 cells, Endoxifen significantly inhibits cell proliferation. Endoxifen also exhibits four-fold higher inhibition on PKC activity compared to tamoxifen.
References: Cancer Chemother Pharmacol. 2005 May;55(5):471-8; Breast Cancer Res Treat. 2010 Jul;122(2):579-84.
Related CAS #: 1032008-74-4 (HCl) 1372937-28-4 (citrate) 1032008-66-4 (acetate) 112093-28-4 (free base) 1032008-71-1 (mesylate)
Chemical Name: (Z)-4-(1-(4-(2-(methylamino)ethoxy)phenyl)-2-phenylbut-1-en-1-yl)phenol hydrochloride
InChi Key: RPFIMPDXTABYCN-BJFQDICYSA-N
InChi Code: InChI=1S/C25H27NO2.ClH/c1-3-24(19-7-5-4-6-8-19)25(20-9-13-22(27)14-10-20)21-11-15-23(16-12-21)28-18-17-26-2;/h4-16,26-27H,3,17-18H2,1-2H3;1H/b25-24-;
SMILES Code: OC1=CC=C(/C(C2=CC=C(OCCNC)C=C2)=C(C3=CC=CC=C3)\CC)C=C1.[H]Cl
Z-Endoxifen HCl; 4-Hydroxy-N-desmethyltamoxifen; Endoxifen hydrochloride; N-Desmethyl-4-hydroxytamoxifen
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
In vitro activity: Endoxifen shows anti-estrogenic effects, and decreases the E2-induced PR expression in MCF-7 cells. Endoxifen also blocks ER-alpha transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation. In MCF7, HS 578T, and BT-549 cells, Endoxifen significantly inhibits cell proliferation. Endoxifen also exhibits four-fold higher inhibition on PKC activity compared to tamoxifen. Endoxifen inhibits the hERG current by preferentially interacting with the activated states of cloned hERG potassium channels with IC50 of 1.6 μM
Cell Assay: MCF7 and Ishikawa cells are grown in 10% triple charcoal-stripped serum-containing medium for 3 d. The cells are then plated at a density of 2,000 cells per well in 96-well tissue culture plates and treated as indicated every 48 h. Cell proliferation assays are conducted 8 days after the first treatment using a CellTiter-Glo Luminescent Cell Viability kit according to the manufacturer's protocol.
Cancer Chemother Pharmacol. 2005 May;55(5):471-8; Breast Cancer Res Treat. 2010 Jul;122(2):579-84.
Purity ≥98%
COA
MSDS