Temsirolimus

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Cat.No. 5264 - Temsirolimus | C56H87NO16 | CAS No. 162635-04-3
Description: mTOR inhibitor; antitumor
Alternative Names: CCI-779
Chemical Name: Rapamycin 42-[3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate]
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature
Pathways

Biological Activity

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

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 103.03 100
ethanol 103.03 100

Preparing Stock Solutions

The following data is based on the product molecular weight 1030.29. Batch specific molecular weights may vary from batch to batch due to solvent 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

Certificate of Analysis / Product Datasheet
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References

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 temsirolimus. 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


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1 Citation for Temsirolimus

Citations are publications that use Tocris products. Selected citations for Temsirolimus include:

Liu (2018) In vivo brain GPCR signaling elucidated by phosphoproteomics. Science 360 eaao4927 PMID: 29930108


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Literature in this Area

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Pathways for Temsirolimus

mTOR

mTOR Signaling Pathway

mTOR is a serine/threonine kinase that nucleates at multiprotein complexes mTORC1 and mTORC2. Signaling by these complexes regulates cell growth, proliferation and survival.