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.

Product Specifications

Molecular Weight

1030.29

Formula

C₅₆H₈₇NO₁₆

Storage

Store at -20°C

Purity

≥98% (HPLC)

Chemical Name

Rapamycin 42-[3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate]

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.

Solubility

	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 all 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	0.10 mL	0.49 mL	0.97 mL
50 mM	0.02 mL	0.10 mL	0.19 mL

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Background References

References are publications that support the biological activity of the product.

Galluzzi Pharmacological modulation of autophagy: therapeutic potential and persisting obstacles. Nat.Rev.Drug.Discov. 2017 PMID: 28529316
Li The novel mTOR inhibitor CCI-779 (temsirolimus) induces antiproliferative effects through inhibition of mTOR in Bel-7402 liver cancer cells. Cancer Cell Int. 2013 PMID: 23537100
Del Bufalo Antiangiogenic potential of the Mammalian target of rapamycin inhibitor temsiro. Cancer Res. 2006 PMID: 16740688
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 PMID: 15805283
Wang 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. 2012 PMID: 22320865

Temsirolimus

Tocris Bioscience, part of Bio-Techne | Catalog # 5264

Key Product Details

Description

Alternative Names

View all mTOR Inhibitors »

Product Description