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Tamoxifen Citrate
54965-24-1
询价 25Kg/Drum 起订
湖北 更新日期:2020-11-10

九州通医药集团股份有限公司

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产品详情:

中文名称:
枸橼酸他莫昔芬
英文名称:
Tamoxifen Citrate
CAS号:
54965-24-1
产品类别:
boshan

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
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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Tamoxifen Citrate;Tamoxifen;

公司简介

九州通是一家以西药、中药、器械为主要经营产品,以医疗机构、批发企业、零售药店为主要客户对象,并为客户提供信息、物流等各项增值服务的大型企业集团。公司立足于医药健康行业,是中国医药商业领域具有全国性网络的少数几家企业之一,于2010年11月2日在上海证券交易所挂牌上市(股票简称:九州通,证券代码:600998),公司连续多年位列中国医药商业企业第四位,领跑中国民营医药商业企业,2020年位列《财富》(中文版)500强第100位。 九州通成立于1999年3月,总部位于湖北省武汉市。截止2020年9月30日,公司注册资本18.78亿元,总资产787.17亿元。实现营业收入803.20亿元,净利润21.41亿元,分别较上年同期增长9.46%和110.23%。扣除非经常性损益后归属于上市公司股东的净利润为12.52亿元,较上年同期增长45.12%。2019年公司实现营业收入994.97亿元,归属于上市公司股东的净利润17.81亿元,分别较上年同期增长14.19%和28.96%。员工两万五千余人。直营和加盟零售连锁药店1074家。

成立日期 (26年)
注册资本 1877663513
员工人数 500人以上
年营业额 ¥ 1亿以上
经营模式 贸易,工厂
主营行业 医药中间体,原料药,兽药原料,维生素类

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