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Temsirolimus

(Synonyms: 替西罗莫司; CCI-779)

目录号: PC15453 纯度: ≥98%

mTOR抑制剂，Temsirolimus 是 mTOR 抑制剂，IC50 值为 1.76 μM。

CAS No. :162635-04-3

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中文名称	Temsirolimus
中文别名	西罗莫司脂化物;替西罗莫司;1,1-二氯-1-氟乙烷;Temsirolimus 抑制剂;坦西莫司;西罗莫司;西罗莫司脂化物 Temsirolimus;西罗莫司脂化物标准品;西罗莫司酯化物;雷帕霉素;坦罗莫司;雷帕霉素42-[3-羟基-2-(羟甲基)-2-甲基丙酸酯];替西莫司;替西罗莫;坦西莫司(替西罗莫司);坦罗莫司(替西罗莫司);坦西莫司, 西罗莫司脂化物
英文名称	Temsirolimus
英文别名	Temsirolimus;Temsirolimus (CCI-779, NSC 683864);42-[3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate]Rapamycin;Temsirolimus (cell cycle inhibitor 779,CCI-779,Torisel®);[14C]-Temsirolimus;CCI779;CCL-779;Rapamycin (42-[3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate];rapaMycin 42-ester with 3-hydroxy-2-(hydroxyMethyl)-2-Methylpropionic acid;TeMsiroliMus (~);TeMsiroliMus (CCI-779,Torisel);TeMsiroliMus (Torisel);CCI-779;Rapamycin 42-[3-Hydroxy-2-(hydroxymethyl)-2-methylpropanoate];C15182;NSC 683864;Temsirolimus(CCI-779);Torisel;624KN6GM2T;42-[3-Hydroxy-2-methylpropanoate;Cci 779;Temserolimus;Temsirolimus - Torisel;Rapamycin 42-(2,2-bis(hydroxymethyl)propionate);DSSTox_CID_20945;DSSTox_RID_79605;DSSTox_GSID_40945;42-(3-Hydroxy-2-(hydroxymethyl)-2-methylpropanoate)rapamycin;Rapamycin 42-[3-hydroxy-2-(hydroxym
Cas No.	162635-04-3
分子式	C₅₆H₈₇NO₁₆
分子量	1030.29
包装储存	4°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
详情描述	mTOR抑制剂，Temsirolimus 是 mTOR 抑制剂，IC50 值为 1.76 μM。

生物活性

Temsirolimus is an inhibitor of mTOR with an IC₅₀ of 1.76 μM. Temsirolimus activates autophagy and prevents deterioration of cardiac function in animal model.

性状

Solid

IC50 & Target[1][2]

mTOR

1.76 μM (IC₅₀)

体外研究(In Vitro)

Temsirolimus potently inhibits mTOR kinase activity with IC₅₀ of 1.76 μM, similar to that of rapamycin with IC₅₀ of 1.74 μM in the absence of FKBP12. Temsirolimus (10 nM to <5 μM) displays a modest and selective antiproliferative activity via FKBP12-dependent mechanism, but can completely inhibit the proliferation of a broad panel of tumor cells at low micromolar concentrations (5-15 μM), involving FKBP12-independent suppression of mTOR signaling. Temsirolimus treatment at micromolar but not nanomolar concentrations (20 μM) causes a marked decline in global protein synthesis and disassembly of polyribosomes, accompanied by rapid increase in the phosphorylation of translation elongation factor eEF2 and the translation initiation factor eIF2A. Temsirolimus inhibits the phosphorylation of ribosomal protein S6, more potently in PTEN-positive DU145 cells than in PTEN-negative PC-3 cells, and inhibits cell growth and clonogenic survival of both cells in a concentration-dependent manner. Temsirolimus (100 ng/mL) potently inhibits proliferation and induces apoptosis in primary human lymphoblastic leukemia (ALL) cells.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

CCI-779 (20 mg/kg, i.p.) inhibits the growth of both prostate cancer xenografts, and the rowth of PC-3 tumors is inhibited in a dose-dependent manner and growth inhibition is greater than for DU145 tumors. In the NOD/SCID xenograft models with human ALL, Temsirolimus treatment at 10 mg/kg/day produces a decrease in peripheral blood blasts and in splenomegaly. Administration of Temsirolimus (20 mg/kg, i.p. 5 days/week) significantly delays the growth of DAOY xenografts by 160% after 1 week and 240% after 2 weeks, compared with controls. Single high-dose of Temsirolimus (100 mg/kg, i.p) treatment induces 37% regression of tumor volume within 1 week. Temsirolimus treatment for 2 weeks also delays the growth of rapamycin-resistant U251 xenografts by 148%. Inhibition of mTOR by Temsirolimus improves performance on four different behavioral tasks and decreases aggregate formation in a mouse model of Huntington disease. Administration of Temsirolimus induces significant dose-dependent, antitumor responses against subcutaneous growth of 8226, OPM-2, and U266 xenografts with ED₅₀ of 20 mg/kg and 2 mg/kg for 8226 and OPM-2, respectively, which are associated with inhibited proliferation and angiogenesis, induction of apoptosis, and reduction in tumor cell size.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

ClinicalTrial

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, 68(8), 2934-2943. [Information]

[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. [Information]

[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. [Information]

[4]. Geoerger B, et al. Antitumor activity of the rapamycin analog CCI-779 in human primitive neuroectodermal tumor/medulloblastoma models as single agent and in combination chemotherapy. Cancer Res, 2001, 61(4), 1527-1532. [Information]

[5]. Ravikumar B, et al. Inhibition of mTOR induces autophagy and reduces toxicity of polyglutamine expansions in fly and mouse models of Huntington disease. Nat Genet. 2004 Jun;36(6):585-95. Epub 2004 May 16. [Information]

[6]. 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. [Information]

[7]. Dela Cruz FS, et al. A case study of an integrative genomic and experimental therapeutic approach for rare tumors: identification of vulnerabilities in a pediatric poorly differentiated carcinoma. Genome Med. 2016 Oct 31;8(1):116. [Information]

[8]. Jason C. Choi, et al. Temsirolimus activates autophagy and ameliorates cardiomyopathy caused by lamin A/C gene mutation. Sci Transl Med. 2012 Jul 25; 4(144): 144ra102. [Information]

溶解度数据

体外研究:

DMSO : 250 mg/mL (242.65 mM; Need ultrasonic)

Ethanol : 200 mg/mL (194.12 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.9706 mL	4.8530 mL	9.7060 mL
5 mM	0.1941 mL	0.9706 mL	1.9412 mL
10 mM	0.0971 mL	0.4853 mL	0.9706 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% EtOH 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 5 mg/mL (4.85 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (4.85 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 EtOH 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% EtOH 90% corn oil
Solubility: ≥ 5 mg/mL (4.85 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (4.85 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 EtOH 储备液加到 900 μL玉米油中，混合均匀。
3.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (2.02 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (2.02 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
4.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (2.02 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (2.02 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

搜索质检报告(COA)

产品使用指南

Data Sheet

[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, 68(8), 2934-2943. [Information]

[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. [Information]

[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. [Information]

[4]. Geoerger B, et al. Antitumor activity of the rapamycin analog CCI-779 in human primitive neuroectodermal tumor/medulloblastoma models as single agent and in combination chemotherapy. Cancer Res, 2001, 61(4), 1527-1532. [Information]

[5]. Ravikumar B, et al. Inhibition of mTOR induces autophagy and reduces toxicity of polyglutamine expansions in fly and mouse models of Huntington disease. Nat Genet. 2004 Jun;36(6):585-95. Epub 2004 May 16. [Information]

[6]. 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. [Information]

[7]. Dela Cruz FS, et al. A case study of an integrative genomic and experimental therapeutic approach for rare tumors: identification of vulnerabilities in a pediatric poorly differentiated carcinoma. Genome Med. 2016 Oct 31;8(1):116. [Information]

[8]. Jason C. Choi, et al. Temsirolimus activates autophagy and ameliorates cardiomyopathy caused by lamin A/C gene mutation. Sci Transl Med. 2012 Jul 25; 4(144): 144ra102. [Information]

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Temsirolimus

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