Everolimus-d4

Everolimus-d4 is the deuterium labeled Everolimus. Everolimus (RAD001) is a Rapamycin 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

[1338452-54-2]

Product Name Alternative

RAD001-d4; SDZ-RAD-d4

UNSPSC

12352005

Hazard Statement

H372

Target

Apoptosis; Autophagy; FKBP; mTOR

Type

Isotope-Labeled Compounds

Related Pathways

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

Field of Research

Cancer

Purity

98.74

Solubility

10 mM in DMSO

Smiles

O=C1N2[C@](CCCC2)([H])C(O[C@](CC([C@@H](/C=C([C@H]([C@H](C([C@@H](C[C@@H](/C=C/C=C/C=C([C@H](C[C@@]3([H])O[C@@](C1=O)([C@@H](CC3)C)O)OC)\C)C)C)=O)OC)O)\C)C)=O)([H])[C@H](C)C[C@H]4C[C@H]([C@@H](CC4)OC([2H])([2H])C([2H])([2H])O)OC)=O

Molecular Formula

C53H79D4NO14

Molecular Weight

962.25

Precautions

H372

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216. |[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]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.|[4]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.|[5]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.