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E-4040 Everolimus, >99%

[Afinitor] [Certican] [RAD001] [SDZ-RAD] [Zortress] [40-O-(2-hydroxyethyl)-rapamycin]

M.W. 958.22

C53H83NO14

[159351-69-6]

M.I. 14:  3907

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 100 mg/mL; soluble in ethanol at 100 mg/mL; very poorly soluble in water; maximum solubility in plain water is estimated to be about 1-10 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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• Everolimus is an immunosuppressant analog of rapamycin (sirolimus) and inhibits growth factor-mediated proliferation of haematopoietic and nonhaematopoietic cells.  Chapman, T.M. and Perry, C.M.  "Everolimus."  Drugs 64:  861-874 (2004).

• Everolimus shows a potent inhibitory effect on posttransplant lymphoproliferative disorder (PTLD)-derived cells in vitro and in vivo, in a dose range that can prevent allograft rejection, and may demonstrate activity in both the prevention and treatment of PTLDs in transplant patients.  Majewski, M., et al.  "Immunosuppressive TOR kinase inhibitor everolimus (RAD) suppresses growth of cells derived from posttransplant lymphoproliferative disorder at allograft-protecting doses."  Transplantation 75:  1710-1717 (2003).

• Oral everolimus inhibits in-stent neointimal growth in the rabbit iliac artery.  Everolimus was well tolerated at a dose of 1.5 mg/kg given 1 day before stenting followed by 0.75 mg/kg per day for 28 days and was related with significant neointimal healing.  Farb, A., et al.  "Oral Everolimus Inhibits In-Stent Neointimal Growth."  Circulation 106:  2379-2384 (2002).

• Everolimus is the active ingredient in the drug sold under the tradenames Afinitor®, Certican®, and Zortress® and in the drug-eluting stent sold under the tradename XienceV®.  The drug has been approved in at least one country for prophylaxis of organ rejection in patients who have received a kidney or heart transplant, and the stent has been approved in at least one country for use in patients undergoing angioplasty.  NOTE:  The everolimus sold by LC Laboratories is NOT Certican® or XienceV®, and is NOT for human use.

• Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.

• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.

• Not available in some countries; not available to some institutions; not available for some uses.

• Please see also our other standard immunosuppressant products:

  A-1040   Ascomycin

  C-6000   Cyclosporin A

  F-4633   Fingolimod, Hydrochloride Salt

  F-4900   FK-506

  P-6040   Pimecrolimus

  R-5000   Rapamycin

  T-8040   Temsirolimus

  T-1377   Tofacitinib, Free Base

  Z-9040   Zotarolimus