[CAS NO. 1032008-74-4] Endoxifen HCl

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PRODUCTS SPECIFICATIONS [1032008-74-4]

Catalog

SLK-S7839

Brand

Selleck

CAS

1032008-74-4

DESCRIPTION [1032008-74-4]

Overview

MDL	-
Molecular Weight	409.95
Molecular Formula	C25H28ClNO2
SMILES	-

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.4393 mL	12.1966 mL	24.3932 mL
5 mM	0.4879 mL	2.4393 mL	4.8786 mL
10 mM	0.2439 mL	1.2197 mL	2.4393 mL
50 mM	0.0488 mL	0.2439 mL	0.4879 mL

Description

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

Targets

Estrogen receptor ^[1]

In vitro

Endoxifen shows anti-estrogenic effects, and decreases the E2-induced PR expression in MCF-7 cells. Endoxifen also blocks ER-alpha transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation. In MCF7, HS 578T, and BT-549 cells, Endoxifen significantly inhibits cell proliferation. Endoxifen also exhibits four-fold higher inhibition on PKC activity compared to tamoxifen. Endoxifen inhibits the hERG current by preferentially interacting with the activated states of cloned hERG potassium channels with IC50 of 1.6 μM.

In vivo

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

References

[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.
[4] Ali SM, et al. Bioorg Med Chem Lett. 2010, 20(8), 2665-2667.
[5] Chae YJ, et al. Eur J Pharmacol. 2015, 752, 1-7.