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Submit ReviewTemsirolimus
Description: mTOR inhibitor; antitumor
Alternative Names: CCI-779
Chemical Name: Rapamycin 42-[3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate]
Purity: ≥98% (HPLC)
Biological Activity for Temsirolimus
Temsirolimus is a mTOR inhibitor; inhibits tumor growth in breast cancer cell lines (IC50 values are 1.6 and 4.3 nM for SKBr3 and BT474, respectively). Inhibits HIF-1α-mediated VEGF production in breast cancer cell lines (BT474 and MDA-MB-231). Directly inhibits serum and VEGF mediated endothelial cell proliferation and morphogenesis in vitro and vessel formation in vivo. Causes G1/S cell cycle arrest in multiple cancer cell lines. Antiangiogenic. Activates autophagy.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Technical Data for Temsirolimus
| M. Wt | 1030.29 |
| Formula | C56H87NO16 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 162635-04-3 |
| PubChem ID | 6918289 |
| InChI Key | CBPNZQVSJQDFBE-FUXHJELOSA-N |
| Smiles | O=C([C@H](C)\C=C([C@@H](O)[C@@H](OC)C([C@@H]4C)=O)/C)C[C@]([C@H](C)C[C@H]2C[C@@H](OC)[C@H](OC(C(CO)(C)CO)=O)CC2)([H])OC([C@@]1([H])N(C(C([C@@]3(O)[C@H](C)CC[C@](C[C@@H](/C(C)=C/C=C/C=C/[C@H](C4)C)OC)([H])O3)=O)=O)CCCC1)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Temsirolimus
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 103.03 | 100 | |
| ethanol | 103.03 | 100 |
Preparing Stock Solutions for Temsirolimus
The following data is based on the product molecular weight 1030.29. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.97 mL | 4.85 mL | 9.71 mL |
| 5 mM | 0.19 mL | 0.97 mL | 1.94 mL |
| 10 mM | 0.1 mL | 0.49 mL | 0.97 mL |
| 50 mM | 0.02 mL | 0.1 mL | 0.19 mL |
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Product Datasheets for Temsirolimus
References for Temsirolimus
References are publications that support the biological activity of the product.
Wang et al (2012) Inhibition of mammalian target of rapamycin signaling by CCI-779 (temsirolimus) induces growth inhibition and cell cycle arrest in Cashmere goat fetal fibroblasts (Capra hircus). DNA Cell Biol. 31 1095 PMID: 22320865
Del Bufalo et al (2006) Antiangiogenic potential of the Mammalian target of rapamycin inhibitor temsiro. Cancer Res. 66 5549 PMID: 16740688
Wu L et al (2005) Effects of the mammalian target of rapamycin inhibitor CCI-779 used alone or with chemotherapy on human prostate cancer cells and xenografts. Cancer Res. 65 2825 PMID: 15805283
Li et al (2013) The novel mTOR inhibitor CCI-779 (temsirolimus) induces antiproliferative effects through inhibition of mTOR in Bel-7402 liver cancer cells. Cancer Cell Int. 13 PMID: 23537100
Galluzzi et al (2017) Pharmacological modulation of autophagy: therapeutic potential and persisting obstacles. Nat.Rev.Drug.Discov. PMID: 28529316
If you know of a relevant reference for Temsirolimus, please let us know.
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Keywords: Temsirolimus, Temsirolimus supplier, Breast, cancer, mTOR, inhibitors, inhibits, rapamycin, kinases, suppresses, cell, tumour, tumor, growth, VEGF, Vascular, endothelial, factor, CCI-779, Cell, Cycle, Inhibitors, Autophagy, 5264, Tocris Bioscience
3 Citations for Temsirolimus
Citations are publications that use Tocris products. Selected citations for Temsirolimus include:
Jun et al (2021) RNA N6-Methyladenosine Methyltransferase METTL3 Facilitates Colorectal Cancer by Activating the m6A-GLUT1-mTORC1 Axis and Is a Therapeutic Target. Gastroenterology 160 1284-1300.e16 PMID: 33217448
Liu (2018) In vivo brain GPCR signaling elucidated by phosphoproteomics. Science 360 eaao4927 PMID: 29930108
Olmez et al (2017) Combined CDK4/6 and mTOR Inhibition Is Synergistic against Glioblastoma via Multiple Mechanisms. Clin Cancer Res 23 6958 PMID: 28814434
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Reviews for Temsirolimus
Average Rating: 5 (Based on 1 Review.)
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Temsirolimus abolishes aversion induced by kappa opioid receptor agonists.
By
Luca Zangrandi on 08/13/2021
Assay Type: In Vivo
Species: Mouse
Conditioned place aversion. Systemic administration
Literature in this Area
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Cancer Metabolism Research Product Guide
This product guide reviews some of the main areas in cancer metabolism research and lists around 150 products that can be used to investigate metabolic pathways in cancer including:
- Glycolysis
- Tricarboxylic Acid Cycle
- Lipidogenesis
- 1C Metabolism and Nucleic Acid Synthesis
- Drivers of Metabolic Reprogramming
- pH and Redox Balance
Cancer Metabolism Poster
This poster summarizes the main metabolic pathways in cancer cells and highlights potential targets for cancer therapeutics. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways providing potential cancer therapeutic targets.
Pathways for Temsirolimus
