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抑制剂/激动剂
囊泡 肿瘤 内分泌与代谢疾病
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PI3K/Akt/mTOR
外泌体 肿瘤生长增殖和凋亡 乳腺癌 前列腺癌 肝癌 结直肠癌 衰老 宫颈癌
/ mTOR / Temsirolimus/替西罗莫司

Temsirolimus/替西罗莫司 {[allProObj[0].p_purity_real_show]}

货号：A642622 同义名： 西罗莫司脂化物 / CCI-779; Torisel

Temsirolimus是一种mTOR抑制剂，IC50为1.76 μM，激活自噬并在动物模型中防止心功能恶化。

Temsirolimus/替西罗莫司 化学结构 CAS号：162635-04-3
Temsirolimus/替西罗莫司 化学结构
CAS号：162635-04-3
Temsirolimus/替西罗莫司 3D分子结构
CAS号：162635-04-3
Temsirolimus/替西罗莫司 化学结构 CAS号：162635-04-3
Temsirolimus/替西罗莫司 3D分子结构 CAS号：162635-04-3
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Temsirolimus/替西罗莫司 纯度/质量文件 产品仅供科研

货号：A642622 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

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产品名称 mTOR ↓ mTORC1 ↓ mTORC2 ↓ 其他靶点 纯度
AZD-8055 ++++

mTOR (full length), IC50: 0.8 nM

mTOR (truncated), IC50: 0.13 nM

 		99%+
Gedatolisib ++++

mTOR, IC50: 1.6 nM

 		99%
GSK1059615 ++

mTOR, IC50: 12 nM

 		98%
Vistusertib +++

mTOR, IC50: 2.8 nM

 		99%+
Torin 1 +++

mTOR, IC50: 4.32 nM

 		+++

mTORC1, IC50: 2 nM

 		++

mTORC2, IC50: 10 nM

 		DNA-PK 99%+
Dactolisib +++

mTOR (p70S6K), IC50: 6 nM

 		98+%
PI-103 +

mTOR, IC50: 30 nM

 		99%+
WAY-600 ++

mTOR, IC50: 9 nM

 		99%
Voxtalisib +

mTOR, IC50: 157 nM

 		99%+
PF-04691502 ++

mTOR, Ki: 16 nM

 		98+%
Onatasertib ++

mTOR, IC50: 16 nM

 		DNA-PK 99%+
Chrysophanol ✔ EGFR 98%
Samotolisib ✔ DNA-PK 99%+
Torkinib +++

mTOR, IC50: 8 nM

 		PDGFR,DNA-PK 99%+
Everolimus 99%+
WYE-354 +++

mTOR, IC50: 5 nM

 		98%
Tacrolimus ✔ 98%
PP121 ++

mTOR, IC50: 13 nM

 		PDGFR,VEGFR 99%+
Torin 2 ++++

mTOR, IC50: 0.25 nM

 		DNA-PK 99%+
Rapamycin ++++

mTOR, IC50: ~0.1 nM

 		98%
GDC-0349 +++

mTOR, Ki: 3.8 nM

 		98%
XL388 ++

mTOR, IC50: 9.9 nM

 		+++

mTORC1, IC50: 8 nM

 		+

mTORC2, IC50: 166 nM

 		99%+
WYE-687 +++

mTOR, IC50: 7 nM

 		98%
Apitolisib +

mTOR, Ki app: 17 nM

 		98%+
WYE-132 ++++

mTOR, IC50: 0.19 nM

 		99%+
Sapanisertib ++++

mTOR, Ki: 1.4 nM

 		99%+
BGT226 maleate ✔ 99%+
ETP-46464 ++++

mTOR, IC50: 0.6 nM

 		DNA-PK 98%
PI3K-IN-1 +

mTOR, IC50: 157 nM

 		98+%
Zotarolimus +++

FKBP-12, IC50: 2.8 nM

 		98%
OSI-027 +++

mTOR, IC50: 4 nM

 		+

mTORC1, IC50: 22 nM

 		+

mTORC2, IC50: 65 nM

 		99%+
Ridaforolimus ++++

mTOR, IC50: 0.2 nM

 		99%+
Temsirolimus +

mTOR, IC50: 1.76 μM

 		95%
CZ415 ++

mTOR, pIC50: 8.07

 		99%+
SF2523 +

mTOR, IC50: 280 nM

 		DNA-PK 99%+
KU-0063794 ++

mTORC1, IC50: ~10 nM

 		++

mTORC2, IC50: ~10 nM

 		99%+
Omipalisib ++++

mTORC1, Ki: 0.18 nM

 		++++

mTORC2, Ki: 0.3 nM

 		99%+
Palomid 529 ✔ 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Temsirolimus/替西罗莫司 生物活性

靶点

  • mTOR

    mTOR, IC50:1.76 μM
描述 mTOR is a serine-threonine kinase that interacts with several proteins to form two distinct complexes, mTORC1 and mTORC2, which show different sensitivities to rapamycin[3]. Temsirolimus (CCI-779, NSC 683864) is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay. Temsirolimus treatment at nanomolar concentrations (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[7]. 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[2]. 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%[5]. In a phase 2 study, 25 mg temsirolimus was intravenously (IV) conducted once per week and the VEGF-A monoclonal antibody bevacizumab 10 mg/kg IV once every 2 weeks in 58 patients with differentiated PNETs and progressive disease by RECIST, results showed response rate (RR) was 41% (23 of 56 patients). PFS at 6 months was 79% (44 of 56). Median PFS was 13.2 months (95%CI,11.2to16.6).Median overall survival was 34 months (95% CI, 27.1 to not reached). For evaluable patients, the most common grade 3 to 4 adverse events attributed to therapy were hypertension (21%), fatigue (16%), lymphopenia (14%), and hyperglycemia (14%), suggesting substantial activity and reasonable tolerability of this drug[6].

Temsirolimus/替西罗莫司 细胞实验

Cell Line
Concentration Treated Time Description References
Caki-1 cells 0.1 μM 24 h B7-H4 gene expression was upregulated Cells. 2022 Apr 25;11(9):1448.
786-O cells 0.1 μM 24 h B7-H4 gene expression was upregulated Cells. 2022 Apr 25;11(9):1448.
A-498 cells 0.1 μM 24 h B7-H4 gene expression was not consistently increased Cells. 2022 Apr 25;11(9):1448.
HEP2 10 μM 2 h and 30 min Temsirolimus induced Akt activation and blocked P70 in HEP2 cells. Br J Cancer. 2007 Mar 26;96(6):952-9.
JN-DSRCT cells 1 mM 9 days To test the effect of Temsirolimus on the proliferation of JN-DSRCT cells, results showed that Temsirolimus significantly inhibited cell proliferation with an IC50 value of 0.042. NPJ Precis Oncol. 2022 Apr 4;6(1):21.
OCI-AML3 cells 2.42 μM 24 h Temsirolimus treatment inhibited p-AKT (Ser473) and p-S6 (Ser240/244), upregulated AKT3, and decreased the expression of total AKT and STAT3. Haematologica. 2017 Sep;102(9):1537-1548.
U937 cells 2.42 μM 24 h Temsirolimus treatment inhibited p-AKT (Ser473) and p-S6 (Ser240/244). Haematologica. 2017 Sep;102(9):1537-1548.
Detroit 562 10 μM 2 h and 30 min Temsirolimus predominantly inhibited P70 in Detroit 562 cells with no significant effects on the phosphorylation of MAPK and/or Akt. Br J Cancer. 2007 Mar 26;96(6):952-9.
H1_DL2 cells 0.05, 5, 10 µM 72 h Combined use of vemurafenib and temsirolimus inhibited tumor cell growth and proliferation in H1_DL2 cells in vitro, compared to single drug treatment, showing a synergistic effect. Int J Mol Sci. 2014 May 16;15(5):8773-94.
H3 cells 0.05, 5, 10 µM 72 h In H3 cells, the combined treatment was less effective compared to H1_DL2 cells, indicating lower sensitivity to the therapy. Int J Mol Sci. 2014 May 16;15(5):8773-94.
MDCKII-Bcrp1 cells 5 μM 60 min To study the inhibitory effect of Temsirolimus on Bcrp1 functional activity, results showed that Temsirolimus significantly increased cellular accumulation of Vandetanib and eliminated its efflux ratio Int J Pharm. 2012 Sep 15;434(1-2):306-14.
MDCK-MDR1 cells 0.5–50μM To study the inhibitory effect of Temsirolimus on P-gp functional activity, results showed that Temsirolimus significantly increased cellular accumulation of [3H]digoxin Int J Pharm. 2012 Sep 15;434(1-2):306-14.

Temsirolimus/替西罗莫司 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice LmnaH222P/H222P mouse model Intraperitoneal injection 5 mg/kg Once daily for two weeks Temsirolimus improved cardiac function in LmnaH222P/H222P mice by inhibiting mTORC1 activity, reducing left ventricular diameters, increasing fractional shortening, and decreasing mRNA levels of atrial natriuretic peptide. Sci Transl Med. 2012 Jul 25;4(144):144ra102
Mice ALL xenograft model Intraperitoneal 5 mg/kg Daily, 5 days a week To evaluate the antitumor effect of Temsirolimus in the ALL xenograft model, results showed that Temsirolimus exhibited some antitumor activity in the ALL xenograft model. Leukemia. 2012 Feb;26(2):271-9
Nude mice HEP2 and Detroit 562 xenograft models Intraperitoneal injection 20 mg/kg Once daily for 28 days Temsirolimus showed significant tumor growth inhibition in both HEP2 and Detroit 562 xenograft models, and synergistic antitumor effects were observed in the Detroit 562 model when combined with an EGFR inhibitor. Br J Cancer. 2007 Mar 26;96(6):952-9.
Mice Lymphoma xenograft model Intraperitoneal 5 mg/kg Every other day for 2 weeks Combined oral metformin and Temsirolimus significantly inhibited lymphoma growth and augmented cell autophagy Cell Death Dis. 2012 Mar 1;3(3):e275
FVB wild type mice Not specified Intravenously 10mg/kg Single dose To study the effect of Temsirolimus on Vandetanib brain penetration, results showed that Temsirolimus had no significant effect on Vandetanib brain uptake Int J Pharm. 2012 Sep 15;434(1-2):306-14.

Temsirolimus/替西罗莫司 动物研究

Dose Mice: 2 mg/kg, 10 mg/kg[3] (i.v.); 0.6 mg/kg[4] (i.p.), 5 mg/kg - 50 mg/kg[2] (i.p.)
Administration i.v., i.p.

Temsirolimus/替西罗莫司 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03629847 Neuroendocrine Tumors Phase 1 Phase 2 Recruiting December 2018 Saudi Arabia ... 展开 >> Oncology Centre, King Faisal Specialist Hospital & Research Center Recruiting Riyadh, Saudi Arabia, 11211 Contact: Ali Aljubran, MD    966-1-4647272 ext 32084    ajubran@kfshrc.edu.sa    Contact: Lani Cabangon, RN    966-1-4647272 ext 32089    lcabangon06@kfshrc.edu.sa    Sub-Investigator: Hussein Raef          Sub-Investigator: Nora Alkahtani, MD          Sub-Investigator: Shouki Bazarbashi, MD          Sub-Investigator: Ahmed Alzahrani, MD          Sub-Investigator: Mohamed Alsubayel, MD          Sub-Investigator: Monther Kabbani, MD          Sub-Investigator: Hamad Albahli, MD          Sub-Investigator: Hadeel Almana, MD 收起 <<
NCT01184326 Solid Tumor K... 展开 >>idney Cancer 收起 << Phase 1 Completed - United States, Massachusetts ... 展开 >> Beth Israel Deaconess Medical Center Boston, Massachusetts, United States, 02115 Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 收起 <<
NCT01184326 - Completed - -

Temsirolimus/替西罗莫司 参考文献

[1]2018:5896786. doi: 10.1155/2018/5896786.

[2]Wu L. 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 Apr 1;65(7):2825-31. doi: 10.1158/0008-5472.CAN-04-3137.

[3]Agostini D. New Insights into the Role of Exercise in Inhibiting mTOR Signaling in Triple-Negative Breast Cancer. Oxid Med Cell Longev. 2018 Sep 30;2018:5896786. doi: 10.1155/2018/5896786.

[4]33(14):1551-6. doi: 10.1200/JCO.2014.56.2082. Epub 2014 Dec 8.

[5]Geoerger B. 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 Feb 15;61(4):1527-32.

Temsirolimus/替西罗莫司 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

0.97mL

0.19mL

0.10mL

4.85mL

0.97mL

0.49mL

9.71mL

1.94mL

0.97mL

Temsirolimus/替西罗莫司 技术信息

CAS号162635-04-3
分子式C56H87NO16
分子量 1030.29
SMILES Code O=C([C@@]1(O)[C@@H](CC[C@@H](C[C@@H](/C(C)=C/C=C/C=C/[C@H](C[C@@H](C)C([C@@H]([C@@H](/C(C)=C/[C@H]2C)O)OC)=O)C)OC)O1)C)C(N3CCCC[C@H]3C(O[C@@H](CC2=O)[C@@H](C[C@@H]4C[C@H]([C@H](OC(C(C)(CO)CO)=O)CC4)OC)C)=O)=O
MDL No. MFCD00934421
别名 西罗莫司脂化物 ;CCI-779; Torisel; Torisel
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C
溶解方案

DMSO: 105 mg/mL(101.91 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 200 mg/mL(194.12 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇

Tags: Temsirolimus | 162635-04-3 | CCI-779 | CCI779 | CCI 779 | mTOR Inhibitor | PI3K/Akt/mTOR | Autophagy | Apoptosis | Anti-infection | mTOR | Autophagy | Apoptosis | Bacterial | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Temsirolimus/替西罗莫司 纯度/质量文件 | Temsirolimus/替西罗莫司 亚型比较 | Temsirolimus/替西罗莫司 生物活性 | Temsirolimus/替西罗莫司 动物研究 | Temsirolimus/替西罗莫司 临床数据 | Temsirolimus/替西罗莫司 参考文献 | Temsirolimus/替西罗莫司 实验方案 | Temsirolimus/替西罗莫司 技术信息

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