| Identification | Back Directory | [Name]
Ridaforolimus (Deforolimus, MK-8669) | [CAS]
572924-54-0 | [Synonyms]
Deforolimus
Ridaforolimus
DeforoliMus API
Ridaforolimus, >
RidaforoliMus, >80%
DeforoliMus(MK-8669)
Deforolimus (AP23573)
deforolimus 572924-54-0
Ridaforolimus (MK-8669)
Deforolimus (AP23573)42-
Ridaforolimus Deforolimus
Deforolimus/MK-8669/AP23573
DeforoliMus (RidaforoliMus)
Deforolimus (AP23573, MK-8669)
42-(Dimethylphosphinate)rapamycin
RapaMycin 42-(DiMethylphosphinate)
RidaforoliMus (DeforoliMus, MK-8669)
RapaMycin,42-(diMethylphosphinate) (9CI)
DeforoliMus(AP 23573,MK-8669,RidaforoliMus)
42-(Dimethylphosphinate)rapamycin USP/EP/BP
Ridaforolimus (Deforolimus, MK8669, AP23573)
AP 23573, MK 8669, 42-DiMethylphosphinate-rapaMycin
Deforolimus, 98%, a potent and selective mTOR inhibitor
AP23573; MK-8669; RIDAFOROLIMUS; AP 23573; MK 8669; AP-23573; MK8669 | [Molecular Formula]
C53H84NO14P | [MOL File]
572924-54-0.mol | [Molecular Weight]
990.214 |
| Questions And Answer | Back Directory | [Description]
Ridaforolimus (Deforolimus, MK-8669, AP23573) is a selective mTOR inhibitor with IC50 of 0.2 nM in HT-1080 cell line; while not classified as a prodrug, mTOR inhibition and FKBP12 binding is similar to rapamycin. Phase 3.
| [Mechanism of action]
Ridaforolimus (also known as AP23573 and MK-8669; formerly known as deforolimus) is an investigational targeted and small-molecule inhibitor of the protein mTOR, a protein that acts as a central regulator of protein synthesis, cell proliferation, cell cycle progression and cell survival, integrating signals from proteins, such as PI3K, AKT and PTEN known to be important to malignancy. Blocking mTOR creates a starvation-like effect in cancer cells by interfering with cell growth, division, metabolism, and angiogenesis.
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| Chemical Properties | Back Directory | [Melting point ]
95-98°C | [Boiling point ]
996.2±75.0 °C(Predicted) | [density ]
1.18±0.1 g/cm3(Predicted) | [storage temp. ]
Hygroscopic, -20?C Freezer, Under Inert Atmosphere | [solubility ]
DMSO (Slightly), Methanol (Slightly) | [form ]
Solid | [pka]
10.40±0.70(Predicted) | [color ]
Off-White to Pale Yellow | [Stability:]
Hygroscopic | [InChIKey]
BUROJSBIWGDYCN-GAUTUEMISA-N |
| Hazard Information | Back Directory | [Chemical Properties]
Off-White Solid | [Uses]
An immunosupressant and is currently being investigated for use in cancer treatments. Ridaforolimus may act as a regulator of protein synthesis, cell proliferation, cell cycle progression and cell survival. Ridaforolimus, was formerly known as Deforolimus. | [Uses]
Ridaforolimus is a semisynthetic macrocyclic lactone prepared from rapamycin by selective alkylation of the 42-hydroxy group with a dimethylphosphinate moiety. Like all tacrolimus analogues, ridaforolimus binds to receptor protein, FKBP12. The complex then binds to mTOR preventing its interaction with target proteins. Ridaforolimus is extensively cited in the literature with over 70 citations. | [Definition]
ChEBI: A semisynthetic derivative that is sirolimus in which hydroxy group attached to the cyclohexyl moiety has been converted to the corresponding dimethylphosphinate. | [Synthesis]
Patent literature summarizes methods for improving rapamycin (sirolimus) fermentation potency (CN101486976A) and high-purity extraction (CN102443012A). The extraction method includes: acetone/ethanol extraction of mycelium; ethyl acetate extraction of sup | [in vivo]
mice bearing mcf7 (breast), pc-3 (prostate), a549 (lung), hct-116 (colon) or panc-1 (pancreas) xenografts have revealed the antitumor efficacy of ridaforolimus [1]. | [IC 50]
mTOR | [References]
[1] rivera vm1, squillace rm, miller d, berk l, wardwell sd, ning y, pollock r, narasimhan ni, iuliucci jd, wang f, clackson t.ridaforolimus (ap23573; mk-8669), a potent mtor inhibitor, has broad antitumor activity and can be optimally administered using intermittent dosing regimens. mol cancer ther. 2011 jun;10(6):1059-71. |
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