TaMoxifen citrate
CAS:54965-24-1
Tamoxifen Citrate is a potent and selective inhibitor of PKC (protein kinase C). It is known that Tamoxifen Citrate functions in PKC ε translocation. Studies suggest that Tamoxifen Citrate functions as an estrogen receptor antagonist in breast tissue. Once bound to the estrogen receptor Tamoxifen Citrate will not allow any other ligand to bind to the receptor. In contrast, Tamoxifen Citrate is an agonist towards this receptor in tissues of the endometrium. Studies indicate Tamoxifen Citrate inhibits DNA synthesis and transcription by recruiting co-repressors, which stop estrogen from interacting with genes. When combined with PAX2, Tamoxifen Citrate can inhibit the proliferation of ERBB2. It is also a high affinity activator of the GPR30 receptor. Tamoxifen Citrate is an activator of Estrogen Receptor.
Common Name |
Tamoxifen citrate |
CAS Number |
54965-24-1 |
Molecular Weight |
563.638 |
Density |
N/A |
Boiling Point |
665.9ºC at 760 mmHg |
Molecular Formula |
C32H37NO8 |
Melting Point |
140-144 °C |
MSDS |
ChineseUSA |
Flash Point |
356.5ºC |
Symbol |
GHS07, GHS08 |
Signal Word |
Danger |
Tamoxifen citrate Biological Activity
Description |
Tamoxifen Citrate is a selective estrogen receptor modulator (SERM). |
Related Catalog |
Signaling Pathways >> Autophagy >> Autophagy
Signaling Pathways >> Others >> Estrogen Receptor/ERR
Research Areas >> Cancer
|
Target |
Estrogen receptor[1]
|
In Vitro |
Tamoxifen shows strong inhibition of MCF-7 cells (EC50=1.41 μM) and to a lesser extent the T47D cells (EC50=2.5 μM) but does not affect the MDA-MB-231 cells[2]. |
In Vivo |
The Tamoxifen-inducible gene knockout strategy has clear advantages in that expression of a gene can be ablated in adult mice at will in a tissue specific manner. To study the role of Med1 in adult heart, 7-week old TmcsMed1-/- mice are given a daily Iintraperitoneal injection of Tamoxifen at a dose of 65 mg/kg for 5 days and killed at selected intervals thereafter. qPCR analysis of RNA shows that the Med1 expression begin to decrease after 3 days of Tamoxifen injection (about 70% decrease), and by 5 days of injection, Med1 expression is almost non-detectable in the heart. Tamoxifen-inducible cardiac-specific disruption of Med1 (TmcsMed1-/-) in adult mice causes dilated cardiomyopathy[3]. |
Animal Admin |
Mice[3] Seven-week old TmcsMed1-/- mice and the wild-type littermates are then administered Tamoxifen intraperitoneally at a daily dose of 65 mg/kg body weight for 5 days and then killed at selected intervals after initiation of Tamoxifen treatment. For each experiment 3 to 5 mice for control and csMed1-/- are used. To obtain survival curve 41 csMed1-/- and 41 csMed1fl/fl mice are used. Thirteen TmcsMed-/- mice and the same number of littermates are used for the survival curve experiments using Tamoxifen inducible model. The specific criteria for animal euthanasia included absence of food or water intake, slow or no mobility, weak or absence of heart beat, absence of palpitation of the chest as well as absence of respiratory movement. Mice are euthanized by intraperitoneal pentobarbital injection at the dose of 150mg/kg body weight to minimize suffering. |
References |
[1]. Osborne CK. Tamoxifen in the treatment of breast cancer. N Engl J Med. 1998 Nov 26;339(22):1609-18.
[2]. Hawariah A, et al. In vitro response of human breast cancer cell lines to the growth-inhibitory effects of styrylpyrone derivative (SPD) and assessment of its antiestrogenicity. Anticancer Res. 1998 Nov-Dec;18(6A):4383-6.
[3]. Jia Y, et al. Cardiomyocyte-Specific Ablation of Med1 Subunit of the Mediator Complex Causes Lethal DilatedCardiomyopathy in Mice. PLoS One. 2016 Aug 22;11(8):e0160755.
|
Chemical & Physical Properties
Boiling Point |
665.9ºC at 760 mmHg |
Melting Point |
140-144 °C |
Molecular Formula |
C32H37NO8 |
Molecular Weight |
563.638 |
Flash Point |
356.5ºC |
Exact Mass |
563.251892 |
PSA |
144.60000 |
LogP |
4.74760 |
Storage condition |
2-8°C |
Water Solubility |
slightly soluble |
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