Ridaforolimus

  • Deforolimus ( USAN )
  • AP23573
  • MK- 8669
  • IUPAC: dimethyl- (1R, 2R, 4S ) -4 - { (2R ) -2 - [ (1R, 9S, 12S, 15R, 16E, 18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18-dihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-2,3,10,14,20-pentaoxo-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraen-12-yl]-propyl}-2-methoxycyclohexylphosphinat
  • 42- dimethylphosphinic - rapamycin

Crystalline powder

Immunosuppressants

  • Insoluble in water
  • Soluble in dimethyl sulfoxide

Template: Infobox chemical / molecular formula search available

Ridaforolimus (also Deforolimus, AP23573 or MK- 8669 ) is an immunosuppressant with a macrolide ( macrocyclic lactone ) and belongs to the class of phosphinic acid. It was developed by Merck in collaboration with ARIAD Pharmaceuticals. It has a close structural relationship to sirolimus ( rapamycin) and tacrolimus ( FK- 506).

Representation

As a basis for the representation of Ridaforolimus serving from the bacterium Streptomyces hygroscopicus derived rapamycin. The hydroxy group of the cyclohexane ring of rapamycin is esterified with Dimethylphosphinsäurechlorid.

Effect

Ridaforolimus inhibits, like the similar rapamycin, the protein mTOR (mammalian Target Of Rapamycin ). This will interfere in the cell proliferation, metabolism, and angiogenesis of cancer cells. It is currently being tested in chemotherapy against bone cancer.

CAS registry number PubChem Immunosuppressive drug Bone tumor National Institutes of Health
683269
de