TargetMol

Endoxifen

Product Code:
 
TAR-T4281
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-T4281-5mg5mg£103.00
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TAR-T4281-10mg10mg£123.00
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TAR-T4281-1mL1 mL * 10 mM (in DMSO)£137.00
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TAR-T4281-30mg30mg£188.00
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TAR-T4281-50mg50mg£256.00
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Further Information

Bioactivity:
(E/Z)-Endoxifen is an active metabolite of tamoxifen produced by the sequential action of cytochrome P450 (CYP) isoforms, including CYP2D6. It is a strong anti-estrogen, as it has an approximately 100-fold greater affinity for estrogen receptors than tamoxifen. As the efficient conversion of tamoxifen to endoxifen depends on CYP2D6, polymorphisms in this CYP isoform can impact the effectiveness of TMX treatment.
CAS:
110025-28-0
Formula:
C25H27NO2
Molecular Weight:
373.496
Pathway:
Endocrinology/Hormones; Microbiology/Virology; Metabolism
Purity:
0.9966
SMILES:
CCC(=C(c1ccc(O)cc1)c1ccc(OCCNC)cc1)c1ccccc1
Target:
Estrogen Receptor/ERR; Aromatase; Estrogen/progestogen Receptor; Parasite; Drug Metabolite

References

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 Mar 1;69(5):1722-7. Wang K, Chen Y, Gao S, et al Norlichexanthone purified from plant endophyte prevents postmenopausal osteoporosis by targeting ER? to inhibit RANKL signaling. Acta Pharmaceutica Sinica B. 2020 Goetz MP, et al. Tamoxifen, endoxifen, and CYP2D6: the rules for evaluating a predictive factor. Oncology (Williston Park). 2009 Dec;23(14):1233-4, 1236. Wang K, Chen Y, Gao S, et al. Norlichexanthone purified from plant endophyte prevents postmenopausal osteoporosis by targeting ER? to inhibit RANKL signaling[J].. Acta Pharmaceutica Sinica B. 2021, 11(2): 442-455