15917-65-4
15917-65-4
Chemical Structure
N-Desmethyltamoxifen hydrochloride
- CAS No.: 15917-65-4
- Formula:C25H28ClNO
- Molecular Weight:393.95
IUPAC Name: (Z)-2-(4-(1,2-diphenylbut-1-en-1-yl)phenoxy)-N-methylethan-1-amine hydrochloride
InChIKey: GMLHJWZEYLTNJW-BJFQDICYSA-N
SMILES: CC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCNC)C=C2)\C3=CC=CC=C3.[H]Cl
Biological Activity: N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
N-Desmethyltamoxifen hydrochloride | 99.63% | N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
N-Desmethyltamoxifen hydrochloride (Standard) | ≥98% | N-Desmethyltamoxifen (hydrochloride) (Standard) is the analytical standard of N-Desmethyltamoxifen (hydrochloride). This product is intended for research and analytical applications. N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
N-Desmethyltamoxifen | 99.59% | N-Desmethyltamoxifen is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Tamoxifen N-oxide | 98.00% | Tamoxifen N-oxide is a Tamoxifen (HY-13757A) metabolite. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Tamoxifen (Standard) | 99.94% | Tamoxifen (Standard) is the analytical standard of Tamoxifen (HY-13757A). This product is intended for research and analytical applications. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively. Tamoxifen activates autophagy and induces apoptosis. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Endoxifen (Z-isomer) | 99.19% | Endoxifen Z-isomer is an orally active selective PKCβ1 inhibitor with an IC50 of 360 nM against human PKCβ1. Endoxifen Z-isomer also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. Endoxifen Z-isomer can be used in research related to ER+ breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Endoxifen (Z-isomer hydrochloride) | 98.98% | Endoxifen Z-isomer hydrochloride is an orally active selective PKCβ1 inhibitor with an IC50 of 360 nM against human PKCβ1. It also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer hydrochloride binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer hydrochloride inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. It can be used in research related to ER+ breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Endoxifen hydrochloride (Standard) | ≥98% | Endoxifen (hydrochloride) (Standard) is the analytical standard of Endoxifen (hydrochloride). This product is intended for research and analytical applications. Endoxifen hydrochloride is a key active metabolite of Tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen hydrochloride has the potential for breast cancer study. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Endoxifen (E-isomer) | 98.02% | Endoxifen E-isomer (E-Endoxifen), an E-isomer of Endoxifen, is an impurity in Endoxifen Z-isomer agent substance. Endoxifen E-isomer exhibits antiestrogenic effects. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Endoxifen (Standard) | ≥98% | Methicillin (sodium hydrate) (Standard) is the analytical standard of Methicillin (sodium hydrate). This product is intended for research and analytical applications. Methicillin sodium hydrate is a narrow-spectrum β-lactam antibiotic, acts by inhibiting penicillin-binding proteins (PBPs). Methicillin sodium hydrate is active against Staphylococcus aureus and Staphylococcus epidermidis that are resistant to other penicillins. Methicillin sodium hydrate can be used for the research of skin infections, osteomyelitis, and endocarditis. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
N-Desmethyl-4′-hydroxytamoxifen | N-Desmethyl-4′-hydroxytamoxifen is an active metabolite of Tamoxifen (HY-13757A). N-Desmethyl-4′-hydroxytamoxifen can be used in breast cancer research. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Tamoxifen-13C6 | Tamoxifen-13C6 (ICI 47699-13C6) is the 13C-labeled Tamoxifen (HY-13757A). Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively. Tamoxifen activates autophagy and induces apoptosis. Tamoxifen also can induce gene knockout of CreER transgenic mouse. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. Vertosick FT Jr, et al. A comparison of the relative chemosensitivity of human gliomas to tamoxifen and n-desmethyltamoxifen in vitro. J Neurooncol. 1994;19(2):97-103. [Content Brief]
- [2]. Morad SA, et al. Modification of sphingolipid metabolism by tamoxifen and N-desmethyltamoxifen in acute myelogenous leukemia--Impact on enzyme activity and response to cytotoxics. Biochim Biophys Acta. 2015 Jul;1851(7):919-28. [Content Brief]
- [3]. Reddel RR,et al. N-desmethyltamoxifen inhibits growth of MCF 7 human mammary carcinoma cells in vitro. Eur J Cancer Clin Oncol. 1983 Aug;19(8):1179-81. [Content Brief]
