2. PI3K/Akt/mTOR Autophagy
  3. mTOR Autophagy
  4. XL388

XL388 is a highly potent and ATP-competitive mTOR inhibitor with an IC50 of 9.9 nM. XL388 simultaneously inhibits both mTORC1 and mTORC2.

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CAS 番号 : 1251156-08-7

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カスタマーレビュー

Based on 4 publication(s) in Google Scholar

XL388 関連抗体

Top Publications Citing Use of Products

    XL388 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 May 2;8(18):30151-30161.  [Abstract]

    786-0 cells are treated with XL388 (500 nM), cells are further cultured in the conditional medium for indicated time, expressions of listed proteins, blot results of three repeats are quantified.

    XL388 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Aug 2;7(31):49527-49538.  [Abstract]

    XL388 inactivates mTORC1/2 in OS cells. Listed OS cells are treated with applied concentration of XL388 for 8 hours, expressions of listed kinases (p- and regular) are tested by Western blots (A, C and D). Kinase phosphorylation is quantified (B). Stable MG-63 cells expressing T308A dominant negative AKT1 (“dnAKT1”) or empty vector (“Vec”, pcDNA3-puro) are treated with or without XL388, cells are further cultured, expressions of listed kinases are tested by Western blots (E), kinase phosphorylat

    mTOR アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    mTOR mTORC1 mTORC2

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    製品説明

    XL388 is a highly potent and ATP-competitive mTOR inhibitor with an IC50 of 9.9 nM. XL388 simultaneously inhibits both mTORC1 and mTORC2.

    IC50 & Target[1]

    mTOR

    9.9 nM (IC50)

    mTORC1

     

    mTORC2

     

    DNA-PK

    8.831 μM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    MCF7 IC50
    1.37 μM
    Compound: 28, XL388
    Antiproliferative activity against human MCF7 cells
    Antiproliferative activity against human MCF7 cells
    		[PMID: 23394126]
    PC-3 IC50
    273 nM
    Compound: 28, XL388
    Inhibition of mTORC1-mediated phosphorylation of S6 at serine 240/244 in human PC3 cells after 3 hrs by ELISA
    Inhibition of mTORC1-mediated phosphorylation of S6 at serine 240/244 in human PC3 cells after 3 hrs by ELISA
    		[PMID: 23394126]
    PC-3 IC50
    330 nM
    Compound: 28, XL388
    Inhibition of mTORC2-mediated phosphorylation of AKT at serine 473 in human PC3 cells after 2 hrs and 50 mins by ELISA
    Inhibition of mTORC2-mediated phosphorylation of AKT at serine 473 in human PC3 cells after 2 hrs and 50 mins by ELISA
    		[PMID: 23394126]
    体外実験

    XL388 (Compound 28) also inhibits DNA-PK with an IC50 of 8.831 μM. XL388 inhibits cellular phosphorylation of mTOR complex 1 (p-p70S6K, pS6, and p-4E-BP1) and mTOR complex 2 (pAKT (S473)) substrates. XL388 acts in an ATP-competitive manner, with a linear increase in IC50 values with increasing ATP concentration[1]. XL388 shows a dose-dependent effect in promoting MG-63 cell apoptosis. XL388 (100 nM) induces apoptosis in other two OS cell lines (U2OS and SaOs-2), but not in non-cancerous MC3T3-E1 cells. XL388 potently inhibits activation of both mTORC1 and mTORC2 in MG-63 cells. The effect of XL388 on mTORC1/2 activation is again dose-dependent. Further, mTORC1/2 activation is almost blocked in XL388 (100 nM)-treated U2OS cells, SaOs-2 cells and primary human OS cells[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    XL388 関連抗体
    体内実験

    To assess the pharmacodynamic effects of XL388 (Compound 28) on the mTOR pathway signaling, athymic nude mice bearing PC-3 prostate tumors are dosed orally at 100 mg/kg of XL388. Rapamycin is also administered intraperitoneally at 5 mg/kg as a reference. Plasma and tumor samples are collected at 1, 4, 8, 16, 24, and 32 h for XL388 and at 4 h for Rapamycin after dosing and homogenized with buffer. Tumor lysates from each animal (n=5) are then pooled for each group and analyzed by immunoblot for levels of phosphorylated p70S6K, S6, 4E-BP1, and AKT. XL388 has moderate terminal elimination half-life (t1/2=1.35 h, 0.45 h, 6.11 h and 0.86 h for mouse (10 mg/kg, iv), rat (3 mg/kg, iv), dog (3 mg/kg, iv), monkey (3 mg/kg, iv))[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    455.50

    分子式

    C23H22FN3O4S
    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(N1CCOC2=CC=C(C3=CC=C(N)N=C3)C=C2C1)C4=CC=C(S(=O)(C)=O)C(F)=C4C
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 50 mg/mL (109.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1954 mL 10.9769 mL 21.9539 mL
    5 mM 0.4391 mL 2.1954 mL 4.3908 mL
    10 mM 0.2195 mL 1.0977 mL 2.1954 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

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    体積 （開始）

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    濃度 （終了）

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
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    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション
    参考文献
    キナーゼ実験
    [1]

    The measurement of mTOR enzyme activity is performed in an ELISA format following the phosphorylation of 4E-BP1 protein. All experiments are performed in the 384-well format. Generally, 0.5 μL of DMSO containing varying concentrations of the test compound is mixed with 15 μL of the enzyme solution. Kinase reactions are initiated with the addition of 15 μL of a solution containing the substrate. The assay conditions are as follows: 0.2 nM mTOR, 10 μM ATP, and 50 nM NHis-tagged 4E-BP1 in 20 mM Hepes, pH 7.2, 1 mM DTT, 50 mM NaCl, 10 mM MnCl2, 0.02 mg/mL BSA, 0.01% CHAPS, 50 mM β-glycerophophate. Following an incubation of 120 min at ambient temperature, 20 μL of the reaction mixture is transferred to a Ni-chelate-coated 384-well plate. The binding step of the 4E-BP1 protein proceeded for 60 min, followed by washing four times each with 50 μL of Tris-buffered saline solution (TBS). Anti-phospho-4E-BP1 rabbit immunoglobulin G (IgG; 20 μL, 1:5000) in 5% BSA-TBST (0.2% Tween-20 in TBS) is added, and the reaction mixuture is further incubated for 60 min. Incubation with a secondary horseradish peroxidase (HRP)-tagged anti-IgG is similarly performed after the primary antibody is washed off (four washes of 50 μL). Following the final wash step with TBST, 20 μL of SuperSignal ELISA Femto is added and the luminescence measured using an EnVision plate reader. Data are reported as the mean (n≥2) [1].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    細胞実験
    [2]

    U2OS, SaOs-2 and MG-63 OS cell lines as well as the murine calvaria-derived osteoblastic MC3T3-E1 cells are maintained and culture. The OB-6 human osteoblastic cells are cultured. For primary culture of murine osteoblasts, the trimmed calvariae of neonatal mice are digested with 0.1% collagenase I and 0.25% dispase. The resolving cell suspensions are neutralized with complete culture medium and are filtered. The calvarial osteoblasts are then resuspended in 10 mL α-MEM containing 15% FBS, and are cultured. Cells (5×104/well) are suspended in 1 mL of DMEM with 1% agar, 10 % FBS and with indicated XL388 (5, 25, 100 and 200nM) treatment. The cell suspension is then added on top of a pre-solidified 1% agar in a 100 mm culture dish. The drug containing medium is refreshed every 2 days. After 10-day incubation, the number of remaining colonies are stained and manually counted[2].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [1]

    Mice, Rats, Dogs and Monkeys[1]
    Pharmacokinetic studies of XL388 are determined in female athymic nude mice, female CD rats, male beagle dogs, and male cynomolgus monkeys. XL388 is administered intravenously and by oral gavage at 10 mg/kg as a solution formulated in EPW (5% ethanol/45% PEG400/water+1:2 HCl (m/m)) to mice, 3 mg/kg as a solution formulated in EPW (5% ethanol/45% PEG400/water+1:2 HCl (m/m)) to CD rats and male beagle dogs, and 3 mg/kg as a solution formulated in EPW (5% ethanol/45% PEG400/water+1:1.5 HCl (m/m)) to male cynomolgus monkeys. The plasma levels of XL388 are monitored over a 24 h period.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1954 mL 10.9769 mL 21.9539 mL 54.8847 mL
    5 mM 0.4391 mL 2.1954 mL 4.3908 mL 10.9769 mL
    10 mM 0.2195 mL 1.0977 mL 2.1954 mL 5.4885 mL
    15 mM 0.1464 mL 0.7318 mL 1.4636 mL 3.6590 mL
    20 mM 0.1098 mL 0.5488 mL 1.0977 mL 2.7442 mL
    25 mM 0.0878 mL 0.4391 mL 0.8782 mL 2.1954 mL
    30 mM 0.0732 mL 0.3659 mL 0.7318 mL 1.8295 mL
    40 mM 0.0549 mL 0.2744 mL 0.5488 mL 1.3721 mL
    50 mM 0.0439 mL 0.2195 mL 0.4391 mL 1.0977 mL
    60 mM 0.0366 mL 0.1829 mL 0.3659 mL 0.9147 mL
    80 mM 0.0274 mL 0.1372 mL 0.2744 mL 0.6861 mL
    100 mM 0.0220 mL 0.1098 mL 0.2195 mL 0.5488 mL
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    XL388 Related Classifications

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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    XL3881251156-08-7XL 388XL-388mTORAutophagyMammalian target of RapamycinInhibitorinhibitorinhibit

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    製品名:
    XL388
    製品番号:
    HY-13806
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