Endoxifen hydrochloride

Endoxifen hydrochloride 是 Tamoxifen 的活性代谢物，是有效的雌激素受体 (estrogen receptor) 拮抗剂。

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库存: 现货

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5mg

￥550.00

440.00

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10mg

￥950.00

760.00

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50mg

￥3050.00

2440.00

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100mg

￥4850.00

3880.00

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货号: ajce56222
CAS: 1197194-41-4
别名: 因多昔芬盐酸盐
分子式: C25H28ClNO2
分子量: 409.95
纯度: >98%
溶解度: DMSO: ≥ 35 mg/mL (85.38 mM); Water: < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

Endoxifen hydrochloride, the active metabolite of Tamoxifen, is a potent antiestrogen that targets estrogen receptor. Estrogen receptor[1]

Endoxifen blocks ER-alpha transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation. These studies reveal that Endoxifen concentrations between 10 and 1000 nM enhance ERα protein degradation. Lower concentrations of Endoxifen (≤1 nM) do not affect ERα protein levels[1].

GLAST::Cre(ERT);ROSA26loxP/loxP mice are injected intraventricularly with 5 μL 5 mM Endoxifen, and mice injected with 4 μL Adeno-Cre virus [109 plaque-forming units (pfu)] serve as positive control. At 7-10 days after ICV injection, mice are sacrificed and the SVZ dissected to isolate and derive stem and progenitor cells. These stem/progenitor cells are then cultured in permissive medium to form neurospheres and assayed for recombination. In our unpassaged preparations is found derived from Endoxifen-injected GLAST::CreERT2;ROSA26loxP/loxP mice that 1.9% of neurospheres show recombination, compared to a higher rate of 4.3% of neurospheres in Adeno-Cre-recombined ROSA26loxP/loxP mice[2].

[1]. Wu X, et al. The tamoxifen metabolite, Endoxifen, is a potent antiestrogen that targets estrogen receptor alpha fordegradation in breast cancer cells. Cancer Res. 2009 Mar 1;69(5):1722-7. [2]. Benedykcinska A, et al.Generation of brain tumours in mice by Cre-mediated recombination of neural progenitors in situ with the tamoxifen metabolite Endoxifen. Dis Model Mech. 2016 Feb;9(2):211-20.