CAS NO: | 1032008-74-4 |
规格: | ≥98% |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
Molecular Weight (MW) | 409.95 |
---|---|
Formula | C25H28ClNO2 |
CAS No. | 1032008-74-4 |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility (In vitro) | DMSO: 74 mg/mL (180.5 mM) |
Water: <1 mg/mL | |
Ethanol: 74 mg/mL (180.5 mM) | |
Other info | 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 |
Synonyms | Z-Endoxifen HCl; 4-Hydroxy-N-desmethyltamoxifen; Endoxifen hydrochloride; N-Desmethyl-4-hydroxytamoxifen |
In Vitro | 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. |
---|---|
In Vivo | In vivo, Endoxifen (8 mg/kg, ) inhibits growth of MCF-7 human mammary tumor xenografts in mice, showing more potency than Tamoxifen. |
Animal model | Mice bearing MCF-7 human mammary tumor xenografts |
Formulation & Dosage | Dissolved in water; 8 mg/kg; Oral gavage |
References | Cancer Chemother Pharmacol. 2005 May;55(5):471-8; Breast Cancer Res Treat. 2010 Jul;122(2):579-84. |