Background
RapaLink-1 is a small-molecule inhibitor of the mammalian target of rapamycin (mTOR), a Ser/Thr protein kinase that functions as an ATP and amino acid sensor to balance nutrient availability and cell growth (1). mTOR inhibitors, such as rapamycin, are used to inhibit the PIK3K-AKT-mTOR pathway, which is a commonly activated pathway in human cancers. RapaLink-1 is an example of a third-generation mTOR inhibitor, which combines the effects of both first-generation (rapamycin and related analogs) and second-generation (MLN0128) mTOR inhibitors (2). Specifically, RapaLink-1 combines the high specificity binding and inhibition of mTORC1 found in rapamycin with the broader specificity of the second-generation mTOR inhibitors, which inhibit both mTORC1 and mTORC2 (3). Several studies have demonstrated that RapaLink-1 can display therapeutic effects in glioblastoma, follicular lymphoma, and renal cell carcinoma, often overcoming resistance to earlier-generation mTOR inhibitors (3-5).
Molecular Formula
C91H138N12O24
Molecular Weight
1784.14 g/mol
Purity
>96%
CAS
1887095-82-0
Solubility
Soluble in DMSO at 178 mg/mL.
Storage
Directions for Use
Background References
Cross-Reactivity Key
H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected
Trademarks and Patents
Limited Uses
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