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(E/Z) -4-Hydroxytamoxifen

CAT: 0804-HY-16950A-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-16950A-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
(E/Z) -4-Hydroxytamoxifen (Afimoxifene) is a racemic compound of (Z) -4-Hydroxytamoxifen and (E) -4-Hydroxytamoxifen isomers. (E/Z) -4-Hydroxytamoxifen is a selective estrogen receptor modulator with mixed estrogenic and antiestrogenic activity, which is also an active metabolite of Tamoxifen. (E/Z) -4-Hydroxytamoxifen is an agonist of the G protein-coupled estrogen receptor (GPER) with relatively low affinity (100-1000 nM). (E/Z) -4-Hydroxytamoxifen is promising for research of cyclical mastalgia, such as breast pain, tenderness, and nodularity[1][2][3][4].
CAS Number
68392-35-8
Product Name Alternative
Afimoxifene; 4-OHT
UNSPSC
12352005
Hazard Statement
H225, H319
Target
Adhesion G Protein-coupled Receptors (AGPCRs) ; Drug Metabolite; Estrogen Receptor/ERR
Type
Reference compound
Related Pathways
GPCR/G Protein; Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor
Applications
Cancer-programmed cell death
Field of Research
Cancer; Metabolic Disease
Assay Protocol
https://www.medchemexpress.com/e-z-4-hydroxytamoxifen.html
Purity
99.62
Solubility
DMSO : 83.33 mg/mL (ultrasonic)
Smiles
OC1=CC=C(/C(C2=CC=C(OCCN(C)C)C=C2)=C(C3=CC=CC=C3)\CC)C=C1
Molecular Formula
C26H29NO2
Molecular Weight
387.51
Precautions
H225, H319
References & Citations
[1]Mansel R, et al. A phase II trial of Afimoxifene (4-hydroxytamoxifen gel) for cyclical mastalgia in premenopausal women. Breast Cancer Res Treat. 2007 Dec;106 (3) :389-97. |[2]Desta Z, et al. Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310 (3) :1062-75.|[3]Gamboa da Costa G, et al. DNA adduct formation and mutant induction in Sprague-Dawley rats treated with tamoxifen and its derivatives. Carcinogenesis. 2001 Aug;22 (8) :1307-15. |[4]Prossnitz ER, et al. International Union of Basic and Clinical Pharmacology. XCVII. G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators. Pharmacol Rev. 2015 Jul;67 (3) :505-40.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3
Isoform
Estrogen receptor; Human Endogenous Metabolite

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