规格

价格

库存

数量

2 mg

¥ 420

5日内发货

生物活性

产品描述	Endoxifen Z-isomer hydrochloride (Endoxifen HCl) is the active metabolite of Tamoxifen, which is an effective and selective estrogen receptor antagonist.
靶点活性	ERG (human):1.6 μM
体外活性	Endoxifen表现出抗雌激素效应，并降低E2诱导的PR表达在MCF-7细胞中。[1] Endoxifen还阻断ER-alpha的转录活性，并抑制由雌激素引起的乳腺癌细胞增殖。[2] 在MCF7、HS 578T和BT-549细胞中，Endoxifen显著抑制细胞增殖。[3] 与tamoxifen相比，Endoxifen在抑制PKC活性方面具有四倍的抑制效果。[4] Endoxifen通过优先与克隆的hERG钾通道的激活状态相互作用，抑制hERG电流，其IC50为1.6 μM。[5]
体内活性	在体内，Endoxifen（8 mg/kg）能够抑制小鼠体内MCF-7人乳腺肿瘤异种移植物的生长，其效力超过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

化学信息

分子量	409.95
分子式	C₂₅H₂₈ClNO₂
CAS No.	1032008-74-4
Smiles	CC/C(=C(\c1ccc(cc1)O)/c1ccc(cc1)OCCNC)/c1ccccc1.Cl
密度	no data available

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

H2O: <1 mg/mL

Ethanol: 69 mg/mL (168.31 mM), Sonication is recommended.

DMSO: 69 mg/mL (168.31 mM), Sonication is recommended.

体内实验配方

10% DMSO+90% Corn Oil: 1.67 mg/mL (4.07 mM), Sonication is recommeded.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

Ethanol/DMSO