Ridaforolimus (Deforolimus, MK-8669) 化学構造
分子量: 990.21



Quality Control & MSDS


  • Compare mTOR Inhibitors
  • 研究分野
  • Combination Therapy



製品説明 Ridaforolimus (Deforolimus, MK-8669) は、0.2nMのIC50による選択的なmTOR阻害剤です。
ターゲット mTOR
IC50 0.2 nM [1]
In vitro試験 Treatment of HT-1080 cells with Deforolimus induces a dose-dependent inhibition of phosphorylation of both S6 and 4E-BP1, with IC50 of 0.2 nM and 5.6 nM, respectively, and leads to a decrease in cell size, an increase in the proportion of cells in the G1 phase of the cell cycle, and inhibition of glucose uptake. Deforolimus displays significant antiproliferative activity a broad panel of cell lines with EC50 of 0.2-2.3 nM. Deforolimus potently and selectively inhibits VEGF production in a dose-dependent manner. [1] Deforolimus treatment significantly induces growth suppression in human NSCLC cell lines with IC30 values of 2.45-8.83 nM, with the exception of H157 with IC30 of >20 nM. Deforolimus treatment (2.8-5.9 nM) significantly dephosphorylates p70S6KThr389 in A549, H1703 and H157 cells, except H1666 that may express a resistant variant of mTORC1, and causes increased phosphorylation of pAKTser473 and pAKTThr308 in A549 and H1703 cells. Deforolimus in combination with the MEK inhibitors, CI-1040 or PD0325901 exhibits dose-dependent synergism in lung cancer cell lines, which is associated with the suppression of proliferation rather than enhancement of cell death, involving the inhibition of ribosomal biogenesis by 40% within 24 hours and a decreased polysome/monosome ratio. [2]
In vivo試験 Administration of Deforolimus exerts significant antitumor effects in mice bearing PC-3 (prostate), HCT-116 (colon), MCF7 (breast), PANC-1 (pancreas) or A549 (lung) xenografts in a dose-dependent manner, and inhibits mTOR signaling in in SK-LMS-1 xenograft model associated with inhibition of tumor growth. [1]

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

Cell based target inhibition HT-1080 cells are treated with increasing concentrations of Deforolimus (0-100 nM) for 2 hours, prior to harvest. Cellular lysates are extracted in denaturing lysis buffer, resolved on SDS-PAGE and transferred to PVDF membranes. After blocking, membranes are incubated with primary antibodies for 1 hour, followed by appropriate HRPconjugated secondary antibodies for 1 hour at room temperature. Immunoreactive proteins are detected using enhanced chemiluminescence and autoradiography performed by exposure to X-ray film. IC50 is determined from the inhibition of levels of phosphorylated ribosomal protein S6 (p-S6) and 4E-BP1 (p-4E-BP1).

細胞アッセイ: [2]

細胞株 Colo205, H1755, H1395, H1666, A549, H157, and H1703 cells
濃度 Dissolved in ethanol, final concentrations ~ 1 μM
反応時間 72-120 hours
実験の流れ Cells are seeded at 2-3 × 104/mL, and serial dilutions of Deforolimus are added after 2 hours, for at least three cell doublings (72-120 hours). Deforolimus effects are measured using the CellTiter 96 Aqueous nonradioactive cell proliferation assay and Sulforhodamine B assays. For Deforolimus, growth effects are described as IC30 because rapamycin and its derivatives do not significantly impede cell proliferation.

動物実験: [1]

動物モデル Male and female athymic NCr-nu mice with xenografts established by subcutaneous implantation of PC-3, A549, HCT-116, MCF7, PANC-1 and SK-LMS-1 tumors
製剤 Dissolved in ethanol, and diluted in a vehicle of 4% ethanol, 5% Tween 80, and 5% propylene glycol
投薬量 ~10 mg/kg
投与方法 Intraperitoneally

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)



Download Ridaforolimus (Deforolimus, MK-8669) SDF
分子量 990.21


CAS No. 572924-54-0
保管 2年-20℃
6月-80℃in solvent
別名 AP23573
溶解度 (25°C) * In vitro DMSO 198 mg/mL (199.95 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol 20 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 42-​(dimethylphosphinate​)-rapamycin

カスタマーフィードバック (1)

Click to enlarge
Source Dr. Zhang of Tianjin Medical University. Ridaforolimus (Deforolimus, MK-8669) purchased from Selleck
Method Western blotting
Cell Lines Breast cancer cells
Concentrations 0-5 nM
Incubation Time 24 h
Results Deforolimus treatment resulted in a reduction of mTOR phosphorylation in Breast cancer cells.

文献中の引用 (4)



電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)


* 必須

Related mTOR 阻害剤

  • MHY1485

    MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits autophagy.

  • CHIR-99021 (CT99021)

    CHIR-99021(CT99021)は、GSK-3αとGSK-3β阻害剤で、IC50 がそれぞれ 10 nM と 6.7 nMである。

  • LY2090314

    LY2090314 は GSK-3α と GSK-3βのために、強力なGSK-3阻害剤で、IC50 がそれぞれ1.5 nM と 0.9 nMです。

  • Afuresertib (GSK2110183)

    Afuresertib (GSK2110183) is a potent, orally bioavailable Akt inhibitor with Ki of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.

  • Rapamycin (Sirolimus)

    Rapamycin (Sirolimus) は、特定のmTOR阻害剤で、IC50 が ~0.1 nMです。

  • Everolimus (RAD001)

    Everolimus (RAD001) は、1.6-2.4nMのIC50によるFKBP12のmTOR阻害剤です。

  • AZD8055


    Features:First drug to inhibit both types of mTOR protein.

  • INK 128 (MLN0128)

    INK 128 (MLN0128)は、有力で選択的なmTOR 阻害剤で、 IC50 が 1 nMです。

  • Torin 1

    Torin1は、mTORの強力な阻害剤で、IC50 が 2-10 nMです。

  • Temsirolimus (CCI-779, NSC 683864)

    Temsirolimus (CCI-779, NSC 683864)は、特定のmTOR阻害剤で、IC50 が 1.76 μM。


Tags: Ridaforolimus (Deforolimus, MK-8669)を買う | Ridaforolimus (Deforolimus, MK-8669)供給者 | Ridaforolimus (Deforolimus, MK-8669)を購入する | Ridaforolimus (Deforolimus, MK-8669)費用 | Ridaforolimus (Deforolimus, MK-8669)生産者 | オーダーRidaforolimus (Deforolimus, MK-8669) | Ridaforolimus (Deforolimus, MK-8669)代理店
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description