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Tamoxifen Citrate

Tamoxifen Citrate

价格: 683

品牌:爱必信

供货周期: 一周

货号:abs817871

规格:>99%

CAS:54965-24-1

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抑制剂描述:

产品名称:Tamoxifen Citrate

产品别名:见爱必信官网

英文别名:Tamoxifen Citrate

靶点:ERR

CAS:54965-24-1

纯度:>99%

外观:见爱必信官网

保存方法:store at -20℃ for one year(Powder); in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述:

Tamoxifen Citrate 是一种抗雌激素,抑制雌激素结合到雌激素受体 (estrogen receptors)。

溶解性:DMSO : 56.4 mg/mL (100 mM)
Ethanol : 2.8 mg/mL (5 mM), with gentle warming

体外研究:

Tamoxifen displays antitumor effect due to its antiestrogenic activity (ER). Values for the apparent affinity of Tamoxifen for the ER range between 30 and 0.01% of that obtained for estradiol, dependent on different ER source (species), protein concentration and condition used for assay. Binding of Tamoxifen to ER further leads to inhibition expression of estrogen-regulated genes, including growth factors and angiogenic factors secreted by the tumor that may stimulate growth by autocrine or paracrine mechanisms. Tamoxifen also directly induces programmed cell death. Tamoxifen produces an inhibitory effect on MCF-7 cell thymidine incorporation and DNA polymerase activity as well as causing a reduction in DNA content of cultures and cell numbers. This inhibitory effect of Tamoxifen on MCF-7 cell growth can be readily reversed by addition of estradiol to the culture medium. 2 and 6 μM Tamoxifen reduces the proportion of cells in S phase and increases the number of cells in G1. At 10 μM, Tamoxifen causes cell death within 48 hr. Tamoxifen inhibits MCF-7 growth with IC50 of ~10 nM after 10 days treatment. Tamoxifen inhibits plasminogen activator activity of MCF-7, and suppresses estradiol-stimulation of plasminogen activator activity. Tamoxifen also evokes minimal increases in cellular progesterone receptor levels. Tamoxifen is able to inhibit the growth of prostate cancer cell PC3, PC3-M, and DU145 with IC50 ranged from 5.5-10 μM, which is related to its inhibition of protein kinase C and induction of p21(waf1/cip1).

体内研究:Tamoxifen administration to rapidly growing, estradiol-stimulated MCF-7 xenografts results in a dose-dependent retardation or cessation of tumor growth by significantly decreasing tumor cell proliferation in tumor. Tamoxifen treatment results in a slowing of tumor growth (tumor doubling time, 12 days), a significant increase in tumor potential doubling time (Tpot) (6.6 days), and a decrease in labeling index (%LI) (to 8%) by 23 days posttreatment, compared with untreated mice which shows a volume doubling time of 5 days, a Tpot of 2.3 days, and a %LI of 23%. Tamoxifen has not only antiestrogenic but also estrogenic properties depending on the species, tissue, and gene. Tamoxifen displays favorable effects on bone and serum lipid concentrations and stimulation endometrium.

产品信息订购:

  产品货号   产品名称   规格 价格 大包装及货期
  abs817871   Tamoxifen Citrate   250mg   683.00   立即咨询
  abs817871   Tamoxifen Citrate   100mg   378.00   立即咨询
  abs817871   Tamoxifen Citrate   500mg   1040.00   立即咨询

产品更多信息请进入爱必信网站咨询




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