Everolimus

• Description :

  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].

• 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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Launched

• Isoform :

  MTORC1