Temsirolimus Inhibitor CAS No. 162635-04-3

Cat. No.	Name	Size	Price
KI0244	Temsirolimus	10 mg	$160
	Temsirolimus	25 mg	$320
	Temsirolimus	50 mg	$560
	Temsirolimus	200 mg	$1900

Chemical Characteristic

Product Name	Temsirolimus
Synonyms	TEM, CCI-779, Torisel
CAS No.	162635-04-3
Molecular Weight	1030.28
Formula	C₅₆H₈₇NO₁₆
Chemical Name	(1R,2R,4S)-4-{(2R)-2-[(3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-dihydroxy-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-1,5,11,28,29-pentaoxo-1,4,5,6,9,10,11,12,13,14,21,22,23,24,25,26,27,28,29,31,32,33,34,34a-tetracosahydro-3H-23,27-ep
Smiles	C(=O)(C(CO)(C)CO)OC1[C@@H](C[C@@H](CC1)C[C@@H](C)C1OC(=O)[C@H]2N(C(=O)C(=O)[C@]3([C@@H](CC[C@@H](C[C@@H](/C(=C/C=C/C=C/[C@H](C[C@H](C(=O)[C@@H]([C@@H](/C(=C/[C@H](C(=O)C1)C)/C)O)OC)C)C)/C)OC)O3)C)O)CCCC2)OC
Chemical Structure

Biological activities

Temsirolimus is a specific inhibitor of mTOR used in the treatment of renal cell carcinoma. The IC50 of temsirolimus against mTOR is 1.76 µM. CCI-779 at low micromolar concentrations broadly suppresses tumor cell proliferation via an FKBP12 (12-kDa FK506-binding protein)-independent mechanism. A CCI-779-resistant mTOR mutant (mTOR-S²⁰³⁵I) displays an 11-fold resistance to the micromolar CCI-779 in vitro with an IC50 of 20 µM. ^[1] In the HER-2 (human epidermal growth factor receptor 2) gene??mplified breast cancer cell line BT474, temsirolimus inhibits vascular endothelial growth factor (VEGF) production in vitro under both normoxic and hypoxic conditions through inhibition of hypoxia-stimulated hypoxia-inducible factor (HIF)-1α expression and transcriptional activation. In addition to its effect on HIF-1α??ediated VEGF production, temsirolimus also directly inhibits serum- and/or VEGF-driven endothelial cell proliferation and morphogenesis in vitro.^[2] Temsirolimus inhibits the migration of endothelial cell (EC) with an IC50 of 50 nM. ^[3] Temsirolimus has antiproliferative activity in three MCL cell lines in a dose- and time-dependent manner. Mechanistically, temsirolimus inhibits mTOR and induces cell-cycle arrest in the G0/G1 phase and a decrease in p21 expression without altering p27 or cyclin D1 levels. ^[4] In vivo, temsirolimus significantly and dose dependently inhibits the proliferation of serum-stimulated HUVEC. Temsirolimus (50 nM) completely inhibits VEGF-stimulated vessel formation. ^[2] Temsirolimus is highly active against malignant pleural mesothelioma (MPM) xenograft models in severe combined immunodeficiency mice as a single agent.^[5]

References

[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] Del Bufalo D, et al. Antiangiogenic potential of the Mammalian target of rapamycin inhibitor temsirolimus.Cancer Res. 2006, 66(11): 5549-5554. [3] Singleton PA et al. Methylnaltrexone potentiates the anti-angiogenic effects of mTOR inhibitors. J Angiogenes Res. 2010, 2(1): 5. [4] Yazbeck VY, et al. Temsirolimus downregulates p21 without altering cyclin D1 expression and induces autophagy and synergizes with vorinostat in mantle cell lymphoma. Exp Hematol. 2008, 36(4): 443-450. [5] Hoda MA, et al. Temsirolimus inhibits malignant pleural mesothelioma growth in vitro and in vivo: synergism with chemotherapy. J Thorac Oncol. 2011, 6(5): 852-863.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.

KareBay^TM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.

About

KareBay^TM Biochem
Sitemap
Blog

Custom Services

Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassry Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services

Biochemical Products

Small Molecule Inhibitors
Bioactive Compounds
Primary Antibodies
Peptides
Amino Acids
Reagents
Fluorescent dyes
Intermediates
PCR

KareBay^TM Biochem, Inc.
11 Deer Park Drive, Suite 102A
Monmouth Junction, NJ 08852

Telephone

: 732-823-1545

Fax

: 732-823-1349

product@karebaybio.com
service@karebaybio.com
support@karebaybio.com