注:本產(chǎn)品僅用于科研,不可用于臨床
Tamoxifen試劑
Tamoxifen (ICI 47699) 是一種口服有效的,選擇性雌激素受體 (estrogen receptor) 調(diào)節(jié)劑 (SERM),可阻斷乳腺細(xì)胞中的雌激素作用,并可激活其他細(xì)胞,如骨骼,肝臟和子宮細(xì)胞中的雌激素活性。Tamoxifen 是一種有效的 Hsp90 激活劑,可增強(qiáng) Hsp90 分子伴侶 ATPase 的活性。Tamoxifen 還可以有效抑制傳染性 EBOV Zaire 和 Marburg (MARV),IC50 分別為 0.1 µM 和 1.8 µM。Tamoxifen 可以激活自噬 (autophagy),誘導(dǎo)凋亡 (apoptosis)。Tamoxifen 還可以誘導(dǎo) CreER(T2) 轉(zhuǎn)基因小鼠的基因敲除。
Tamoxifen試劑 生物活性
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[1][2][3]. 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[5]. Tamoxifen activates autophagy and induces apoptosis[4]. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse[6].
體外研究 (In Vitro) | Tamoxifen (ICI 47699) 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||||||
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體內(nèi)研究 (In Vivo) | Injection of pre-mutant mice with Tamoxifen (75 mg/kg; injected for 5 days at 6 weeks of age) results in the excision of the floxed exon and, thus, in a gene knockout[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||||||
分子量 | 371.51 | ||||||||||||||||
性狀 | Solid | ||||||||||||||||
Formula | C26H29NO | ||||||||||||||||
CAS 號(hào) | 10540-29-1 | ||||||||||||||||
中文名稱 | 三苯氧胺;它莫西芬 | ||||||||||||||||
運(yùn)輸條件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
儲(chǔ)存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) | ||||||||||||||||
溶解性數(shù)據(jù) | In Vitro: DMSO : 50 mg/mL (134.59 mM; Need ultrasonic) Ethanol : 50 mg/mL (134.59 mM; Need ultrasonic) 配制儲(chǔ)備液
* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。 In Vivo: 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨?。以下溶解方案都?qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑: ——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用; 以下溶劑前顯示的百
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