Endoxifen Z-isomer hydrochloride
作者：齐岳
发布时间：2023-08-25
08:58:39
点击数：
产品名称：Endoxifen Z-isomer hydrochloride
产品描述：
| 产品描述 | Endoxifen HCl is the active metabolite of Tamoxifen, which is an effective and selective estrogen receptor antagonist. |
| 靶点活性 | hERG:1.6 μM |
| 体外活性 | Endoxifen shows anti-estrogenic effects, and decreases the E2-induced PR expression in MCF-7 cells. [1] Endoxifen also blocks ER-alpha transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation. [2] In MCF7, HS 578T, and BT-549 cells, Endoxifen significantly inhibits cell proliferation. [3] Endoxifen also exhibits four-fold higher inhibition on PKC activity compared to tamoxifen. [4] Endoxifen inhibits the hERG current by preferentially interacting with the activated states of cloned hERG potassium channels with IC50 of 1.6 μM. [5] |
| 体内活性 | In vivo, Endoxifen (8 mg/kg, ) inhibits growth of MCF-7 human mammary tumor xenografts in mice, showing more potency than Tamoxifen. [3] |
| 细胞实验 | 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.(Only for Reference) |
| 别名 | Z-因多昔芬盐酸盐, Endoxifen HCl |
| 分子量 | 409.95 |
| 分子式 | C25H28ClNO2 |
| CAS No. | 1032008-74-4 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: <1 mg/mL
Ethanol: 69 mg/mL (168.3 mM)
DMSO: 69 mg/mL (168.3 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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