| Description | Endoxifen hydrochloride, a principal active metabolite of Tamoxifen (TAM), exhibits heightened affinity and specificity towards the estrogen receptor and possesses aromatase inhibitory capability. It holds promise for breast cancer research. |
| In vitro | Endoxifen，Tamoxifen的一个羟基化代谢物，是雌激素受体(ER)拮抗剂。此外，与4-羟基Tamoxifen不同，Endoxifen在抑制ER的转录作用外，还能促使乳腺癌细胞中ER-α的降解。[1] Endoxifen是一种强效抗雌激素物质，促进乳腺癌细胞中雌激素受体α的降解。研究还表明，Endoxifen能够阻碍ERA的转录活性，并有效抑制即使在Tamoxifen、N-去甲基-Tamoxifen和4-羟基Tamoxifen存在下的乳腺癌细胞雌激素诱导的增殖。[2] Endoxifen在所有乳腺癌细胞线中以10 μM浓度显示出显著的生长抑制作用，但对MDAMB-468细胞线的抑制作用中等。在10 μM浓度下，特别是在MCF7、HS 578T和BT-549细胞中观察到明显的细胞毒性作用。相比之下，较低浓度的Endoxifen(0.01-1 μM)的抑制效果不如10 μM显著。然而，100 μM的Endoxifen浓度对所有测试细胞均致命。[2] |
| In vivo | Endoxifen口服给药后迅速吸收并容易进入全身循环。连续28天每日一次口服Endoxifen，剂量为2、4、8 mg/kg，在雌性小鼠中显示出安全性并逐渐抑制人类乳腺肿瘤异种移植物的生长。[2] |
| molecular weight | 409.95 |
| Molecular formula | C25H28ClNO2 |
| CAS | 1197194-41-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | H2O: 0.9 mg/mL (2.2 mM), Sonication and heating to 80℃ are recommended. DMSO: 55 mg/mL (134.16 mM), Sonication is recommended. |
| References | 1. Goetz MP. Tamoxifen, endoxifen, and CYP2D6: the rules for evaluating a predictive factor. Oncology (Williston Park). 2009;23(14):1233-1236. 2. Wu X, et al. The tamoxifen metabolite, endoxifen, is a potent antiestrogen that targets estrogen receptor alpha for degradation in breast cancer cells. Cancer Res. 2009;69(5):1722-1727. 3. Gingery A, et al. The effects of a novel hormonal breast cancer therapy, endoxifen, on the mouse skeleton. PLoS One. 2014;9(5):e98219. |