Ridaforolimus (Deforolimus, MK-8669)

Ridaforolimus (Deforolimus, MK-8669) は、0.2nMのIC50による選択的なmTOR阻害剤です。

目録号S1022
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Ridaforolimus (Deforolimus, MK-8669) 化学構造
分子量: 990.21

品質と確認

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Quality Control & MSDS

製品情報

  • Combination Therapy
    併用療法
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    mTOR阻害剤を比較
  • 研究分野

製品の説明

生物活性

情報 Ridaforolimus (Deforolimus, MK-8669) は、0.2nMのIC50による選択的なmTOR阻害剤です。
目標 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]
臨床試験
特集

推薦された実験操作 (公開の文献だけ)

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]

細胞系 Colo205, H1755, H1395, H1666, A549, H157, and H1703 cells
濃度 Dissolved in ethanol, final concentrations ~ 1 μM
処理時間 72-120 hours
方法 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
管理 Intraperitoneally
Solubility 30% PEG400/0.5% Tween80/5% propylene glycol, 20 mg/mL
* 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.

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

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
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)
1

参考

化学情報

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

C53H84NO14P

CAS No. 572924-54-0
保管 2年-20℃
6月-80℃in DMSO
別名 N/A
溶解度 (25°C) * In vitro DMSO 198 mg/mL (199 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

研究分野

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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.

製品表彰状 (5)

技術サポート&よくある質問(FAQ)

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