Endoxifen Z-isomer hydrochloride

Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.

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库存: 现货

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1mg

￥387.00

310.00

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5mg

￥687.00

550.00

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10mg

￥925.00

740.00

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50mg

￥0.00

0.00

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100mg

￥0.00

0.00

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货号: ajce56224
CAS: 1032008-74-4
别名: Z-因多昔芬盐酸盐
分子式: C25H28ClNO2
分子量: 409.95
纯度: >98%
溶解度: DMSO: 12.5 mg/mL (30.49 mM); Water: < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.

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]

In vivo, Endoxifen (8 mg/kg, ) inhibits growth of MCF-7 human mammary tumor xenografts in mice, showing more potency than Tamoxifen. [3]

[1] Lim YC, et al. Cancer Chemother Pharmacol. 2005, 55(5), 471-478. [2] Wu X, et al. Cancer Res. 2009, 69(5), 1722-1727. [3] Ahmad A, et al. Breast Cancer Res Treat. 2010, 122(2), 579-584.