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Temsirolimus

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[8].

Product Specifications

CAS Number

[162635-04-3]

Product Name Alternative

CCI-779

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Autophagy; Bacterial; mTOR

Type

Reference compound

Related Pathways

Anti-infection; Apoptosis; Autophagy; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Temsirolimus.html

Purity

99.56

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C56H87NO16

Molecular Weight

1030.29

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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.|[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.|[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.|[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.|[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.|[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.|[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.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, protect from light, stored under nitrogen)

Scientific Category

Reference compound1

Clinical Information

Launched

Isoform

MTORC1

Available Sizes

Curated Selection

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