R8781 Sigma


Ready Made Solution, 2.5 mg/mL in DMSO (2.74 mM), from Streptomyces hygroscopicus

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



Related Categories Approved Therapeutics/Drug Candidates, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Pfizer Compounds,
Quality Level   PREMIUM
biological source   from Streptomyces hygroscopicus
sterility   0.2 μm filtered
assay   ≥95% (HPLC)
form   solution
concentration   2.5 mg/mL in DMSO (2.74 mM)
Mode of action   enzyme | inhibits
antibiotic activity spectrum   fungi
originator   Pfizer
storage temp.   −20°C


Biochem/physiol Actions

Rapamycin is a macrocyclic triene antibiotic possessing potent immunosuppressant and anticancer activity. It forms a complex with FKBP12 that binds to and inhibits the molecular target of rapamycin (mTOR). mTOR is a member of the phosphoinositide kinase-related kinase (PIKK) family that enhances cellular proliferation via the phosphoinositol 3-kinase/Akt signaling pathway. Inhibition of this pathway by rapamycin blocks downstream elements that result in cell cycle arrest in G1. The effectors of mTOR action include 4EBP1 and S6K1.

Other Notes

Rapamycin has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the Rapamycin probe summary on the Chemical Probes Portal website.

Features and Benefits

This compound is featured on the Phosphoinositide Kinases 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

Safety & Documentation

Safety Information

NA 1993 / PGIII
WGK Germany 
Flash Point(F) 
188.6 °F
Flash Point(C) 
87 °C


Certificate of Analysis

Certificate of Origin

Protocols & 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

Phosphoinositide Kinases

The membranes of all metazoan cells contain a substantial amount of phosphatidylinositol (PtdIns) and at least seven phosphorylated PtdIns derivatives (PPIn) at 30- to 1000-fold lower concentrations....
Keywords: Cancer, Catalysis, Gene expression, Genetic, Growth factors, Phosphorylations

Peer-Reviewed Papers


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