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Temsirolimus

产品编号 T2145 CAS 162635-04-3

别名: NSC 683864, CCI-779, 西罗莫司脂化物

Temsirolimus (CCI-779) 是一种mTOR 抑制剂，IC50值为 1.76 μM。它能激活自噬，可防止心脏功能恶化。

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Temsirolimus, CAS 162635-04-3

规格	价格/CNY	货期
2 mg	￥ 313	现货
5 mg	￥ 472	现货
10 mg	￥ 738	现货
25 mg	￥ 1,430	现货
50 mg	￥ 2,280	现货
100 mg	￥ 3,730	现货
500 mg	￥ 7,880	现货

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纯度: 100%

纯度: 99.64%

纯度: 97.76%

纯度: 97.69%

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生物活性

化学信息

存储 & 溶解度

参考文献

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产品描述	Temsirolimus (CCI-779) is a specific mTOR inhibitor ( IC50: 1.76 μM), used in the treatment of advanced renal cell cancer.
靶点活性	mTOR:1.76 μM (cell free)
体外活性	Temsirolimus (CCI-779; 10 nmol/L to <5 μmol/L) exhibited a generally flat and cell-selective inhibition of cell proliferation. The most sensitive cell lines that were inhibited by ≥50% included LNCap, PC3MM2, MDA468, H446, and Caco2, whereas those with ≤25% inhibition were SW480, HT29, HCT116, and H460 [1]. Following a 3-day exposure to 100 nmol/L CCI-779, the numbers of colony-forming PC-3 and DU145 cells were 0.18 ± 0.09 and 0.37 ± 0.03, respectively, compared with controls [2].
体内活性	The growth of PC-3 tumors was inhibited by CCI-779 in a dose-dependent manner and growth inhibition was greater than for DU145 tumors. Mean delay in growth to a volume of 500 mm3 was 39 ± 5 and 17 ± 3 days, respectively, following treatment with CCI-779 (20 mg/kg i.p.) five times weekly for 3 weeks. Mice were randomized to treatment with 5 to 10 mg/kg/d of CCI-779 or vehicle alone as a control [2]. Mice were treated 6 days per week. A statistically significant improvement in disease burden was seen in all samples tested. Mice xenografted from 3 of the patients (96, 240, and 359) had a statistically significant decrease in splenic disease bulk [3]. CCI-779, given as 10 intraperitoneal injections, induced significant dose-dependent, antitumor responses against subcutaneous growth of 8226, OPM-2, and U266 cell lines. Effective doses of CCI-779 were associated with modest toxicity, inducing only transient thrombocytopenia and leukopenia. Although CCI-779-mediated inhibition of the p70 mTOR substrate was equal in 8226 and OPM-2 tumor nodules, OPM-2 tumor growth was considerably more sensitive to inhibition of proliferation, angiogenesis, and induction of apoptosis [4].
激酶实验	The Flag-tagged wild-type human mTOR (Flag-mTOR) and Flag-mTOR-SI (S2035I, created by site-directed mutagenesis) DNA constructs were transiently transfected into HEK293 cells. Protein extraction and purification of Flag-mTOR and Flag-mTOR-SI were carried out 48 h later as described previously. In vitro kinase assays of purified Flag-mTOR and Flag-mTOR-SI without or with FKBP12 were done and detected by dissociation-enhanced lanthanide fluorescent immunoassay (DELFIA) as described [1].
细胞实验	For all experiments, cells were plated in six-well plates in complete growth media for overnight. Various doses of CCI-779 or rapamycin analogs were added alone or with FK506 for indicated periods of time. Total cellular lysates were prepared using NuPAGE-LDS sample buffer. Equal amounts of proteins were subjected to immunoblotting analysis using NuPAGE electrophoresis system. Immunoblots were probed with appropriate primary and secondary antibodies following the manufacturer's instructions and detected using enhanced chemiluminescence. β-Actin immunoblotting and/or reversible Ponceau-S staining of nitrocellulose membranes after the transfer was used to visualize the total protein loading [1].
动物实验	Mice bearing PC-3 tumors were treated with CCI-779 (1, 5, 10, and 20 mg per kg per day), or vehicle solution for 3 or 5 days per week for 3 weeks. Mice bearing DU145 tumors were only treated with CCI-779 (20 mg per kg per day) or vehicle solution for 3 weeks. Mice bearing PC-3 tumors received the following treatments: (a) control, vehicle solution for CCI-779; (b) chemotherapy alone, mitoxantrone 1.5 mg/kg or docetaxel 10 mg/kg was injected i.p. weekly for 3 doses; (c) CCI-779 alone, 5 or 10 mg/kg was injected i.p. daily, three times a week for 3 weeks; (4) chemotherapy followed by CCI-779. The largest and perpendicular diameters of tumors were measured twice weekly, and animals were coded using ear tags so that the observer was unaware of their treatment history. Tumor volume was estimated and plotted against time to evaluate response to treatment [2].

别名	NSC 683864, CCI-779, 西罗莫司脂化物
分子量	1030.29
分子式	C56H87NO16
CAS No.	162635-04-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 70 mg/mL (67.9 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
Ethanol	1 mM	0.9706 mL	4.853 mL	9.706 mL	24.265 mL
	5 mM	0.1941 mL	0.9706 mL	1.9412 mL	4.853 mL
	10 mM	0.0971 mL	0.4853 mL	0.9706 mL	2.4265 mL
	20 mM	0.0485 mL	0.2427 mL	0.4853 mL	1.2133 mL
	50 mM	0.0194 mL	0.0971 mL	0.1941 mL	0.4853 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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容积 (起始)

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参考文献

1. Shor B, et al. A new pharmacologic action of CCI-779 involves FKBP12-independent inhibition of mTOR kinase activity and profound repression of global protein synthesis. Cancer Res. 2008 Apr 15;68(8):2934-43. 2. Wu L, et al. Effects of the mammalian target of rapamycin inhibitor CCI-779 used alone or with chemotherapy on human prostate cancer cells and xenografts. Cancer Res, 2005, 65(7), 2825-2831. 3. Teachey DT, et al. The mTOR inhibitor CCI-779 induces apoptosis and inhibits growth in preclinical models of primary adult human ALL. Blood, 2006, 107(3), 1149-1155. 4. Frost P, et al. In vivo antitumor effects of the mTOR inhibitor CCI-779 against human multiple myeloma cells in a xenograft model. Blood. 2004 Dec 15;104(13):4181-7. Epub 2004 Aug 10.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Temsirolimus 162635-04-3 Apoptosis Autophagy PI3K/Akt/mTOR signaling mTOR Inhibitor NSC-683864 CCI 779 NSC 683864 Mammalian target of Rapamycin NSC683864 CCI779 CCI-779 inhibit 西罗莫司脂化物 inhibitor

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Temsirolimus

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

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