Description Mechanism of action
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42-(Dimethylphosphinate)rapamycin

Description Mechanism of action
42-(Dimethylphosphinate)rapamycin Structure
42-(Dimethylphosphinate)rapamycin
  • CAS No.572924-54-0
  • Chemical Name:42-(Dimethylphosphinate)rapamycin
  • CBNumber:CB72462148
  • Molecular Formula:C53H84NO14P
  • Formula Weight:990.21
  • MOL File:572924-54-0.mol
42-(Dimethylphosphinate)rapamycin Property
  • 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)
  • pka 10.40±0.70(Predicted)
  • form Solid
  • color Off-White to Pale Yellow
  • Stability Hygroscopic
  • FDA UNII 48Z35KB15K
  • NCI Dictionary of Cancer Terms ridaforolimus
  • NCI Drug Dictionary ridaforolimus
  • ATC code L01EG03
  • UNSPSC Code 12352200
  • NACRES NA.77
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H373-H400
  • Precautionary statements P273-P391-P501-P260-P314-P501

42-(Dimethylphosphinate)rapamycin Chemical Properties,Usage,Production

  • 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.

  • Description MK-8669 is a rapamycin analog that selectively inhibits mTOR (IC50 = 0.2 nM). Like rapamycin, MK-8669 binds FKBP12 to form a complex that associates with the FKBP-rapamycin binding domain on mTOR and allosterically inhibits mTORC1 kinase activity. MK-8669 is more water soluble than rapamycin and is amenable to oral or intravenous administration. Formulations containing rapalogs, including MK-8669, have promise against a subset of cancers, including advanced kidney cancer. MK-8669 is also being examined for effectiveness against cancers when used in combination with other chemotherapeutic compounds.
  • 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. Potent mTORC1 inhibitor.
  • 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.
  • 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.
42-(Dimethylphosphinate)rapamycin Preparation Products And Raw materials
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42-(Dimethylphosphinate)rapamycin Spectrum
572924-54-0, 42-(Dimethylphosphinate)rapamycinRelated Search:
  • API
  • Pharmaceuticals
  • Intermediates & Fine Chemicals
  • Inhibitors
  • PI3K
  • mTOR
  • Akt
  • 药靶配体
  • 合成有机化合物配体
  • 科研试剂
  • 细胞生物学试剂
  • 原料药
  • 小分子抑制剂，天然产物
  • 抑制剂
  • 微生物代谢物
  • 原料药中间体
  • C53H84NO14P
  • RIDAFOROLIMUS (DEFOROLIMUS, MK-8669) |CAS 572924-54-0
  • 化合物RIDAFOROLIMUS,10 MM DMSO 溶液
  • (1R,2R,4S)-4-((R)-2-((3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34AS)-9,27-二羟基-10,21-二甲氧基-6,8,12,14,20,26-六甲基-1,5,11,28,29-五氧代-1,4,5,6,9,10,11,12,13,14,21,22,23,24,25,26,27,28,29,31,32,33,34,34A-二十四氢-3H-23,27-环氧吡啶并[2,1-C][1]氮杂环三十一烷-3-基)丙基)-
  • MK-8669; DEFOROLIMUS; AP23573
  • RIDAFOROLIMUS (DEFOROLIMUS, MK-8669),药雷帕霉素
  • 利达福莫司
  • 化合物RIDAFOROLIMUS
  • (二甲基亚膦酰)雷帕霉素合成)
  • 42-(二甲基亚膦酰)雷帕霉素, 一种有效和选择性MTOR抑制剂
  • RIDAFOROLIMUS DEFOROLIMUS
  • MTOR抑制剂(DEFOROLIMUS)
  • 药雷帕霉素
  • (二甲基亚膦酰)雷帕霉素
  • 42-(二甲基亚膦酰)雷帕霉素
  • 雷帕霉素衍生物
  • 572924-54-0
  • (1R,2R,4S)-4-[(2R)-2-[(1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28Z,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,
  • RIDAFOROLIMUS DRUG SUBSTANCE
  • Ridaforolimus, 10 mM in DMSO
  • (1R,2R,4S)-4-((R)-2-((3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,27-Dihydroxy-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-1,5,11,28,29-pentaoxo-1,4,5,6,9,10,11,12,13,14,21,22,23,24,25,26,27,28,29,31,32,33,34,34a-tetracosahydro-3H-23,27-epoxypyrido[2,1-c][1]oxa[4]azacyclohentriacontin-3-yl)propyl)-2-methoxycyclohexyl dimethylphosphinate
  • Deforolimus/MK-8669/AP23573
  • Ridaforolimus
  • Ridaforolimus (MK-8669)
  • Ridaforolimus (Deforolimus, MK8669, AP23573)
  • 42-(Dimethylphosphinate)rapamycin USP/EP/BP
  • Ridaforolimus, &gt
  • Ridaforolimus Deforolimus
  • Deforolimus, 98%, a potent and selective mTOR inhibitor
  • deforolimus 572924-54-0
  • AP23573; MK-8669; RIDAFOROLIMUS; AP 23573; MK 8669; AP-23573; MK8669
  • Deforolimus (AP23573)
  • Deforolimus (AP23573, MK-8669)
  • Deforolimus
  • 42-(Dimethylphosphinate)rapamycin
  • Deforolimus (AP23573)42-
  • RapaMycin,42-(diMethylphosphinate) (9CI)
  • AP 23573, MK 8669, 42-DiMethylphosphinate-rapaMycin
  • RapaMycin 42-(DiMethylphosphinate)
  • DeforoliMus(MK-8669)
  • DeforoliMus API
  • RidaforoliMus (DeforoliMus, MK-8669)

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