Everolimus (RAD001) , ≥98% , 159351-69-6

CAS NO.：159351-69-6

Empirical Formula: C53H83NO14

Molecular Weight: 958.22

MDL number: MFCD00929329

EINECS: 621-003-9

PRODUCT Properties

• Melting point: NA
• Boiling point: 998.7±75.0 °C(Predicted)
• Density: 1.18±0.1 g/cm3(Predicted)
• Flash point: 2℃
• storage temp.: -20°C
• solubility: Soluble in DMSO (up to 100 mg/ml) or in Ethanol (up to 100 mg/ml).
• form: solid
• pka: 10.40±0.70(Predicted)
• color: White
• Water Solubility: Soluble in dimethysulfoxide,ethanol and chloroform. Slightly soluble in water.
• Stability: Hygroscopic
• InChIKey: HKVAMNSJSFKALM-GKUWKFKPSA-N

Description and Uses

Everolimus, an oral immunosuppressant for the treatment of kidney and heart transplant rejection, is the 40-O-(2-hydroxyethyl) derivative of rapamycin. It has immunosuppressive properties similar to those of rapamycin, but with improved pharmacokinetic profile. Everolimus, like rapamycin, is a proliferation signal inhibitor that exerts its immunosuppressive effect by inhibiting the activation of p70 S6 kinase, thereby blocking growth factor-driven proliferation of T cells, B cells and vascular smooth muscle cells, and arresting cell cycle at the G1 phase. Inhibition of p70 S6 kinase activation by everolimus and rapamycin is mediated by their binding to FKBP12 (FK506 binding-protein 12). Everolimus inhibits FK506 binding to FKBP12 with an IC50 of 1.8–2.6 nM, and it is about 3- to 5-fold less potent than rapamycin (IC50=0.4–0.9 nM). The in vitro immunosuppressive activity of everolimus is also slightly less than that of rapamycin as demonstrated in a mixed lymphocyte reaction (MLR) assay (IC50=0.2–1.6 nM versus 0.07–0.5 nM, respectively) and in antigen-specific human helper T-cell clones (IC50=0.05–0.17nM versus 0.014–0.37nM, respectively). However, the in vivo immunosuppressive activity of oral everolimus 1–5 mg/ kg/day is similar to that of rapamycin at equivalent doses in rat models of renal or cardiac transplantation, localized graft-versus-host disease, and autoimmune glomerulonephritis. The recommended dosage of everolimus is 0.75 mg twice daily, and it is used in combination with cyclosporine microemulsion and corticosteroids.

Macrolide immunosuppressant; derivative of Rapamycin. Inhibits cytokine-mediated lymphocyte proliferation

Safety

• Symbol(GHS): GHS08,GHS09
• Signal word: Warning
• Hazard statements: H351-H361fd-H373-H410
• Precautionary statements: P202-P260-P273-P280-P308+P313-P391
• Hazard Codes: T,Xn,F
• Risk Statements: 48/25-36-20/21/22-11
• Safety Statements: 45-36/37-26-16
• RIDADR: UN 1648 3 / PGII
• WGK Germany: 2
• F: 10
• HS Code: 29349990
• Hazardous Substances Data: 159351-69-6(Hazardous Substances Data)