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R0395 Sigma

Rapamycin from Streptomyces hygroscopicus

≥95% (HPLC), powder

Synonym: 23,27-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine, AY 22989, Sirolimus

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Description

Frequently Asked Questions

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Biochem/physiol Actions

A macrocyclic triene antibiotic that binds to and inhibits the molecular target of rapamycin (mTOR). It forms a complex with FKBP12 that binds to and inhibits the molecular target of rapamycin (mTOR). Rapamycin is a potent immunosuppressant and has anticancer activity.

Packaging

1 mg in glass bottle

Features and Benefits

This compound is featured on the PKB/Akt page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

This compound was developed by Pfizer. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Protocols & Applications

Antibiotic Selector for application, solubility, solution stability, working concentration, and mode of action information

Price and Availability


DISCOVER Bioactive Small Molecules
Safety & Documentation
Protocols & Articles

Articles

Discover Bioactive Small Molecules for Immunology Research

The immune system is a complex network to detect and defend against non-self pathogenic agents, such as disease-causing viruses, bacteria, and other microorganisms. Various signaling pathways contrib...
Keywords: Antibiotics, Antifungals, Antivirals, Apoptosis, Bioactive small molecules, Cell signaling, Diabetes, Diseases, Immunology, Inflammation

Oncogenes and Tumor Suppressors Reprogram Metabolism

Proliferating cells require the biosynthesis of structural components for biomass production and for genomic replication. This requires a reprogramming of the metabolic pathways to ensure nutrients s...
Keywords: Aerobic, Antitumor agents, Apoptosis, Biofiles, Cancer, Citric Acid Cycle, Degradations, Environmental, Events, Gene expression, Glycolysis, Growth factors, Metabolic Pathways, Metabolism, Metabolites, Nucleotide Synthesis, PAGE, Pentose phosphate pathway, Phosphorylations, Support

The Cancer Stem Cell Hypothesis

Traditionally, cancer has been viewed as a disease in which environmental or endogenous events induce mutations to critical oncogenes and tumor suppressor genes within a normal cell. The clinical man...
Vicki Caligur
BioFiles 2008, 3.5, 4.
Keywords: Angiogenesis, Apoptosis, Asymmetric synthesis, Cancer, Catalysis, Cell culture, Cell division, Cell proliferation, Clinical, DNA replication, Degradations, Eliminations, Environmental, Events, Gastrointestinal, Gene expression, Growth factors, Ligands, Metabolic Pathways, Phosphorylations, Poisons, Transcription, Transfection, transformation

Peer-Reviewed Papers

References

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Degradation Of Regulator Of Calcineurin 1 (RCAN1) Is Mediated By Both Chaperone-mediated Autophagy And Ubiquitin Proteasome Pathways. Liu, H., et al. FASEB J. 23, 3383-92, (2009)

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Rapamycin reverses cellular phenotypes and enhances mutant protein clearance in Hutchinson-Gilford Progeria Syndrome cells. Cao, K. et al. Sci. Transl. Med. 3, (2011)

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TOR Complex 2 Controls Gene Silencing, Telomere Length Maintenance, And Survival Under DNA-damaging Conditions. Schonbrun, M., et al. Mol. Cell. Biol. 29, 4584-94, (2009)

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mTOR as a positive regulator of tumor cell responses to hypoxia. Abraham, R.T. Curr. Top. Microbiol. Immunol. 279, 299-319, (2004)

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Integration of growth factor and nutrient signaling: implications for cancer biology. Shamji, A.F., et al. Mol. Cell. 12, 271-280, (2003)

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Targeting the mTOR signaling network in cancer Chiang GG, and Abraham RT. Trends Mol. Med. 13, 433-442, (2007)

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Upstream of the mammalian target of rapamycin; do all roads pass through mTOR? Corradetti MN, and Guan KL. Oncogene 25, 6347-6360, (2006)

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From The Cover: Bifurcation Of Insulin Signaling Pathway In Rat Liver: MTORC1 Required For Stimulation Of Lipogenesis, But Not Inhibition Of Gluconeogenesis Li, S., et al. Proc. Natl. Acad. Sci. U. S. A. 107, 3441-3446, (2010)

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Involvement of PI3K/Akt/TOR pathway in stretch-induced hypertrophy of myotubes. Sasai, N., et al. Muscle Nerve 41, 100-6, (2010)

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Targeting mTOR with rapamycin; One dose does not fit all Foster DA, Toschi A. Cell Cycle 2, 8, (2009)

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The molecular target of rapamycin (mTOR) as a therapeutic target against cancer. Mita, MM, et al. Cancer Biol. Ther. 2, S169-S177, (2003)

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The molecular target of rapamycin (mTOR) as a therapeutic target against cancer. Mita, MM, et al. Cancer Biol. Ther. 2, S169-S177, (2003)

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Biosynthesis And Expression Of VE-cadherin Is Regulated By The PI3K/mTOR Signaling Pathway. Bieri, M., et al. Mol. Immunol. 46, 866-72, (2009)

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Monitoring The Autophagy Pathway In Cancer. Dorsey, F.C., et al. Meth. Enzymol. 453, 251-71, (2009)

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Enhanced Longevity by Ibuprofen, Conserved in Multiple Species, Occurs in Yeast through Inhibition of Tryptophan Import. He C, Tsuchiyama SK, Nguyen QT, et al. PLoS Genet. 10(12), e1004860, (2014)

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Rapamycin: in vitro profile of a new immunosuppressive macrolide. Sehgal, S.N. and Bansback, C.C. Ann. N. Y. Acad. Sci. 685, 58-67, (1993)

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Minimally invasive direct coronary artery bypass improves late survival compared with drug-eluting stents in isolated proximal left anterior descending artery disease: a 10-year follow-up, single-center, propensity score analysis. Benedetto U, Raja SG, Soliman RF, et al. J. Thorac. Cardiovasc. Surg. 148(4), 1316-22, (2014)

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Everolimus-eluting stents or bypass surgery for multivessel coronary disease. Bangalore S, Guo Y, Samadashvili Z, et al. N. Engl. J. Med. 372(13), 1213-22, (2015)

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A direct method for the measurement of everolimus and sirolimus in whole blood by LC-MS/MS using an isotopic everolimus internal standard. Morgan PE, Brown NW, Tredger JM, et al. Ther. Drug Monit. 36(3), 358-65, (2014)

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Nonmyeloablative allogeneic hematopoietic stem cell transplantation for GATA2 deficiency. Grossman J, Cuellar-Rodriguez J, Gea-Banacloche J, et al. Biol. Blood Marrow Transplant. 20(12), 1940-8, (2014)

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FR104, an antagonist anti-CD28 monovalent fab' antibody, prevents alloimmunization and allows calcineurin inhibitor minimization in nonhuman primate renal allograft. Poirier N, Dilek N, Mary C, et al. Am. J. Transplant. 15(1), 88-100, (2014)

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A retrospective 15-year review: survival advantage after switching to sirolimus in hepatitis C virus infected liver graft recipients. Shah M, Shankar A, Gee I, et al. Aliment. Pharmacol. Ther. 41(4), 379-92, (2015)

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Insights into autophagosome maturation revealed by the structures of ATG5 with its interacting partners. Kim JH, Hong SB, Lee JK, et al. Autophagy 11(1), 75-87, (2015)

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Rapamycin and chloroquine: the in vitro and in vivo effects of autophagy-modifying drugs show promising results in valosin containing protein multisystem proteinopathy. Nalbandian A, Llewellyn KJ, Nguyen C, et al. PLoS ONE 10(4), e0122888, (2015)

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Berberine alleviates ox-LDL induced inflammatory factors by up-regulation of autophagy via AMPK/mTOR signaling pathway. Fan X, Wang J, Hou J, et al. J. Transl. Med. 13, 92, (2015)

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Improved oral absorption and chemical stability of everolimus via preparation of solid dispersion using solvent wetting technique. Jang SW, Kang MJ, et al. Int. J. Pharm. 473(1-2), 187-93, (2014)

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Chronic rapamycin treatment causes diabetes in male mice. Schindler CE, Partap U, Patchen BK, et al. Am. J. Physiol. Regul. Integr. Comp. Physiol. 307(4), R434-43, (2014)

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The effect of mammalian target of rapamycin inhibition on T helper type 17 and regulatory T cell differentiation in vitro and in vivo in kidney transplant recipients. Kim KW, Chung BH, Kim BM, et al. Immunology 144(1), 68-78, (2015)

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Extracorporeal membrane oxygenation support after pediatric orthotopic heart transplantation. Su JA, Kelly RB, Grogan T, et al. Pediatr. Transplant. 19(1), 68-75, (2014)

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The risk of recurrent IgA nephropathy in a steroid-free protocol and other modifying immunosuppression. Von Visger JR, Gunay Y, Andreoni KA, et al. Clin. Transplant. 28(8), 845-54, (2014)

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Safety and efficacy of colistin versus meropenem in the empirical treatment of ventilator-associated pneumonia as part of a macro-project funded by the Seventh Framework Program of the European Commission studying off-patent antibiotics: study protocol for a randomized controlled trial. Rosso-Fernández C, Garnacho-Montero J, Antonelli M, et al. Trials 16, 102, (2015)

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Nicorandil prevents sirolimus-induced production of reactive oxygen species, endothelial dysfunction, and thrombus formation. Aizawa K, Takahari Y, Higashijima N, et al. J. Pharmacol. Sci. 127(3), 284-91, (2015)

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Reduced sirolimus systemic exposure and improved bioresorbable polymer properties: new allies for the treatment of patients with coronary artery disease. Stojkovic S, Neskovic AN, Mehmedbegovic Z, et al. Fundam. Clin. Pharmacol. 29(1), 95-105, (2015)

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Effects of the mTOR inhibitor rapamycin on monocyte-secreted chemokines. Lin HY, Chang KT, Hung CC, et al. BMC Immunol. 15, 37, (2015)

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Diabetes mellitus and renal transplantation in adults: is there enough evidence for diagnosis, treatment, and prevention of new-onset diabetes after renal transplantation? Suarez O, Pardo M, Gonzalez S, et al. Transplant. Proc. 46(9), 3015-20, (2014)

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Rapid and sensitive UPLC-MS-MS determination of tacrolimus in Wistar rats and human blood. Upadhyay V, Trivedi V, Shah G, et al. J. Chromatogr. Sci. 52(1), 59-67, (2013)

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Three vs twelve months of dual antiplatelet therapy after zotarolimus-eluting stents: the OPTIMIZE randomized trial. Feres F, Costa RA, Abizaid A, et al. JAMA 310(23), 2510-22, (2013)

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Results of an international randomized phase III trial of the mammalian target of rapamycin inhibitor ridaforolimus versus placebo to control metastatic sarcomas in patients after benefit from prior chemotherapy. Demetri GD, Chawla SP, Ray-Coquard I, et al. J. Clin. Oncol. 31(19), 2485-92, (2013)

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Mitonuclear protein imbalance as a conserved longevity mechanism. Houtkooper RH, Mouchiroud L, Ryu D, et al. Nature 497(7450), 451-7, (2013)

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Biodegradable polymer biolimus-eluting stent versus durable polymer everolimus-eluting stent: a randomized, controlled, noninferiority trial. Natsuaki M, Kozuma K, Morimoto T, et al. J. Am. Coll. Cardiol. 62(3), 181-90, (2013)

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Everolimus for women with trastuzumab-resistant, HER2-positive, advanced breast cancer (BOLERO-3): a randomised, double-blind, placebo-controlled phase 3 trial. André F, O'Regan R, Ozguroglu M, et al. Lancet Oncol. 15(6), 580-91, (2014)

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Phase II study of temsirolimus (CCI-779) in women with recurrent, unresectable, locally advanced or metastatic carcinoma of the cervix. A trial of the NCIC Clinical Trials Group (NCIC CTG IND 199). Tinker AV, Ellard S, Welch S, et al. Gynecol. Oncol. 130(2), 269-74, (2013)

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Dominant-activating germline mutations in the gene encoding the PI(3)K catalytic subunit p110δ result in T cell senescence and human immunodeficiency. Lucas CL, Kuehn HS, Zhao F, et al. Nat. Immunol. 15(1), 88-97, (2014)

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Safety and efficacy outcomes of first and second generation durable polymer drug eluting stents and biodegradable polymer biolimus eluting stents in clinical practice: comprehensive network meta-analysis. Navarese EP, Tandjung K, Claessen B, et al. BMJ 347, f6530, (2013)

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Inhibition of the mTORC pathway in the antiphospholipid syndrome. Canaud G, Bienaimé F, Tabarin F, et al. N. Engl. J. Med. 371(4), 303-12, (2014)

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Effect of visceral metastases on the efficacy and safety of everolimus in postmenopausal women with advanced breast cancer: subgroup analysis from the BOLERO-2 study. Campone M, Bachelot T, Gnant M, et al. Eur. J. Cancer 49(12), 2621-32, (2013)

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Third-generation zotarolimus-eluting and everolimus-eluting stents in all-comer patients requiring a percutaneous coronary intervention (DUTCH PEERS): a randomised, single-blind, multicentre, non-inferiority trial. von Birgelen C, Sen H, Lam MK, et al. Lancet 383(9915), 413-23, (2014)

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Needs for monitoring mosquito transmission of malaria in a pre-elimination world. James S, Takken W, Collins FH, et al. Am. J. Trop. Med. Hyg. 90(1), 6-10, (2014)

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Systematic characterization of the conformation and dynamics of budding yeast chromosome XII. Albert B, Mathon J, Shukla A, et al. J. Cell Biol. 202(2), 201-10, (2013)

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RTOG 0913: a phase 1 study of daily everolimus (RAD001) in combination with radiation therapy and temozolomide in patients with newly diagnosed glioblastoma. Chinnaiyan P, Won M, Wen PY, et al. Int. J. Radiat. Oncol. Biol. Phys. 86(5), 880-4, (2013)

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