Endoxifen - 4OHNDtam | N-Desmethyl-4-hydroxytamoxifen

Based on 14 reference(s) in Google Scholar 8 10 14

Axon 2190

CAS [110025-28-0]

MF C25H27NO2
MW 373.49

Purity: 99%
Soluble in 0.1N HCl(aq) and DMSO

Endoxifen

Description

Metabolite of Tamoxifen and a selective estrogen receptor modulator (SERM); Potently inhibits the growth of estrogen-stimulated BT474 cells (IC50: 54 nM). Approximately 100-fold more potent as an antagonist of the ERα than the parent drug. Drug for the treatment of estrogen receptor (ER) positive breast cancer.
The water soluble hydrochloride salt Endoxifen hydrochloride is available as Axon 2707. The more active isomer, Z-Endoxifen, is available as Axon 2221.

J.R. Hawse et al. Endoxifen’s Molecular Mechanisms of Action Are Concentration Dependent and Different than That of Other Anti-Estrogens. PLoS One. 2013, 8, e54613.

A Ahmad et al. Endoxifen, a New Cornerstone of Breast Cancer Therapy: Demonstration of Safety, Tolerability, and Systemic Bioavailability in Healthy Human Subjects. Clin. Pharmacol. Ther. 2010, 88(6), 814–817.

M.D. Johnson et al. Pharmacological Characterization of 4-hydroxy-N-desmethyl Tamoxifen, a Novel Active Metabolite of Tamoxifen. Breast Cancer Research and Treatment 2004, 85, 151-159.

M. Goetz et al. Tamoxifen, HER2, and Endoxifen: The Role of CYP2D6 as a Predictor of Tamoxifen Resistance in ER+/HER2+ Breast Cancer. Cancer Res 2009, 69, Abstract nr 2006 (S3).

Selective estrogen receptor modulator (SERM)

Chemical name

(E/Z)-4-(1-(4-(2-(methylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenol

Parent CAS No.

[110025-28-0]

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Size	Unit Price	Stock
10 mg	€125.00	In Stock
50 mg	€450.00	In Stock

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Size	Unit Price	Stock
2 x 10 mg	€200.00	In Stock

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Related Products

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1898	ERB 041	Selective estrogen receptor β (ERβ) agonist	€95.00
1926	Estetrol	Estrogen receptor agonist (four- to five-fold preference for the Erα)	€130.00
2221	(Z)-Endoxifen	The more active (Z)-isomer of Endoxifen (SERM; Axon 2190)	€150.00
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2652	ZB716	Steroidal, orally bioavailable SERD	€130.00
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2790	BHPI	ER-α antagonist	€125.00
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3650	Clomiphene citrate	Selective estrogen receptor modulator (SERM)	€50.00
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4093	(Z)-4-Hydroxytamoxifen	The more active metabolite of Tamoxifen (SERM; Axon 3252)	€110.00
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Endoxifen - 4OHNDtam | N-Desmethyl-4-hydroxytamoxifen

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Endoxifen - 4OHNDtam | N-Desmethyl-4-hydroxytamoxifen

Description

Chemical name

Parent CAS No.

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