Everolimus

Everolimus (RAD001) is a Rapamycin (HY-10219) derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities[1][2].

Product Specifications

CAS Number

[159351-69-6]

Product Name Alternative

RAD001; SDZ-RAD

UNSPSC

12352005

Hazard Statement

H351, H361, H373, H410

Target

Apoptosis; Autophagy; Bacterial; FKBP; mTOR

Type

Reference compound

Related Pathways

Anti-infection; Apoptosis; Autophagy; Cell Cycle/DNA Damage; Immunology/Inflammation; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

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

Concentration

10mM

Purity

99.85

Solubility

DMSO : 50 mg/mL (ultrasonic; warming; heat to 60°C)

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](OCCO)CC4)OC)C)=O)=O

Molecular Formula

C53H83NO14

Molecular Weight

958.22

Precautions

H351, H361, H373, H410

References & Citations

[1]O'Reilly T, et al. Biomarker Development for the Clinical Activity of the mTOR Inhibitor Everolimus (RAD001) : Processes, Limitations, and Further Proposals. Transl Oncol. 2010 Apr;3 (2) :65-79.|[2]Lane HA, et al. mTOR inhibitor RAD001 (everolimus) has antiangiogenic/vascular properties distinct from a VEGFR tyrosine kinase inhibitor. Clin Cancer Res, 2009, 15 (5), 1612-1622.|[3]Zhu Y, et al. Antitumor effect of the mTOR inhibitor Everolimus on human breast cancer stem cells in vitro and in vivo. Tumour Biol. 2012 Oct;33 (5) :1349-62.|[4]Kawata T, et al. Dual inhibition of the mTORC1 and mTORC2 signaling pathways is a promising therapeutic target for adult T-cell leukemia. Cancer Sci. 2018 Jan;109 (1) :103-111.