1. PI3K/Akt/mTOR
  2. mTOR
  3. RMC-5552

RMC-5552 is a potent and selective mTORC1 inhibitor. RMC-5552 inhibits phosphorylation of mTORC1 pS6K and p4EBP1 with IC50s of 0.14 nM and 0.48 nM, respectively. RMC-5552 shows much lower pAKT inhibition (IC50 of 19 nM), resulting in mTORC1/mTORC2 selectivity approaching 40-fold. RMC-5552 has anti-cancer activity.

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CAS 番号 : 2382768-62-7

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 5476 在庫あり
Solution
10 mM * 1 mL in DMSO USD 5476 在庫あり
Solid
1 mg $580 在庫あり
5 mg $1750 在庫あり
10 mg $2800 在庫あり
25 mg $5600 在庫あり
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100 mg   お問い合わせ  

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カスタマーレビュー

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    RMC-5552 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Dec 24:2025.12.22.696045.  [Abstract]

    Immunoblots from the indicated PTEN-deficient T-ALL cells treated for 48 hrs with MPA (1 μM) with or without the mTORC1 inhibitor RMC-5552 (1 nM) or the AKT inhibitor MK-2206 (2 μM) in CCRF-CEM cells.

    RMC-5552 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Jul 17:2025.07.11.663903.  [Abstract]

    Immunoblot analysis for phospho-4EBP1 S65, phospho-4EBP1 T37/T46, phosphor-S6K 235/236, 4 hours and 24 hours post RMC-5552 treatment from 0.1-100nM dose range across tRCC cell lines.

    RMC-5552 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Dec 24:2025.12.22.696045.  [Abstract]

    Immunoblots from the indicated PTEN-deficient T-ALL cells treated for 48 hrs with MPA (1 μM) with or without the mTORC1 inhibitor RMC-5552 (1 nM) or the AKT inhibitor MK-2206 (2 μM) in MOLT-3 cells.

    RMC-5552 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Jul 17:2025.07.11.663903.  [Abstract]

    Immunoblot analysis for CyclinD1 after 72 hours of RMC-5552 treatment from 0.1nM- 100nM dose range across tRCC cell lines.

    RMC-5552 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Dec 24:2025.12.22.696045.  [Abstract]

    Immunoblots on indicated cells treated for 24 hrs with MPA (1 μM) with or without RMC-5552 (1 nM) or MK-2206 (2 μM) in CCRF-CEM and MOLT-3 cells.

    RMC-5552 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Dec 24:2025.12.22.696045.  [Abstract]

    Indicated cells treated for 72 hrs with MPA (2.5 μM) with or without RMC-5552 (1 nM). Cell death was quantified by Annexin V/ Propidium Iodide (AV/PI) staining, and graphed as percent of the total cell population.

    RMC-5552 purchased from MedChemExpress. Usage Cited in: Blood Neoplasia. 2024 Apr 30;1(2):100015.

    NPRL2-WT or -KO NALM-6 cells were treated for 72 hours with either DMSO, dexamethasone, RMC-5552, or a combination of dexamethasone and RMC-5552, and cell viability was assessed.

    mTOR アイソフォーム固有の製品をすべて表示:

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

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    製品説明

    RMC-5552 is a potent and selective mTORC1 inhibitor. RMC-5552 inhibits phosphorylation of mTORC1 pS6K and p4EBP1 with IC50s of 0.14 nM and 0.48 nM, respectively. RMC-5552 shows much lower pAKT inhibition (IC50 of 19 nM), resulting in mTORC1/mTORC2 selectivity approaching 40-fold. RMC-5552 has anti-cancer activity[1].

    IC50 & Target[1]

    mTORC1

     

    体外実験

    The presence of FKBP12, whose recruitment would only be observed in the presence of the FKBP12-FRB allosteric modality of RMC-5552. Density for RMC-5552 is evident at the interface between FKBP12 and the FRB domain of mTOR. RMC-5552 makes hydrogen bonds to the backbone of G2238 and V2240, the “hinge” of mTOR, via the 4-aminopyrazolo[3,4-d]pyrimidine core, and the 2-aminobenzoxazole makes hydrogen-bonding interactions to E2190 and K2187[1].

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

    体内実験

    RMC-5552 (1-10 mg/kg; i.p.; once weekly; for 28 days) exhibits antitumor activity in a human xenograft model of MCF-7 breast cancer in mice in vivo[1].
    PK Parameters of RMC-5552 38 in Mice at 1 mg/kg via IP Administration[1]

    compounds Tmax (h) Cmax (ng/mL) Cmax (μM) AUClast (μg/mL × h) AUClast (μM × h) t1/2 (h)
    38 RMC-5552 2.0 ± 0.0 5667 ± 1106 3.19 ± 0.62 46 089 ± 5320 25.9 ± 3.0 4.8 ± 0.4

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

    Animal Model: Female Balb/c nude mice (6-8 weeks of age) injected with MCF-7 cells[1]
    Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg
    Administration: i.p.; once weekly; for 28 days
    Result: Resulted in a reduction in tumor volume.
    臨床実験
    分子量

    1778.13

    分子式

    C93H136N10O24

    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    NC1=C(C2=NC=N1)C(C3=CC=C(O4)C(N=C4N)=C3)=NN2CC5=CC=C(C6)C(CCN6C(CCOCCOCCOCCOCCOCCOCCOCCOCCNC(O[C@H](CC[C@H]7C[C@H]([C@@](C[C@H]([C@@H](/C=C([C@H]([C@H](C([C@@H](C[C@@H]8C)C)=O)OC)O)\C)C)O)([H])OC([C@@](CCCC9)([H])N9C(C([C@](O[C@]%10([H])C[C@@H](/C(C)=C/C=C/C=C/8)OC)([C@@H](CC%10)C)O)=O)=O)=O)C)[C@@H](C7)OC)=O)=O)=C5

    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 : ≥ 100 mg/mL (56.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.5624 mL 2.8119 mL 5.6239 mL
    5 mM 0.1125 mL 0.5624 mL 1.1248 mL
    10 mM 0.0562 mL 0.2812 mL 0.5624 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    一般には略語で表示されます:C1V1 = C2V2

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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: 5 mg/mL (2.81 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% Corn Oil

      Solubility: 5 mg/mL (2.81 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    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.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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

    純度: 99.94%

    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 0.5624 mL 2.8119 mL 5.6239 mL 14.0597 mL
    5 mM 0.1125 mL 0.5624 mL 1.1248 mL 2.8119 mL
    10 mM 0.0562 mL 0.2812 mL 0.5624 mL 1.4060 mL
    15 mM 0.0375 mL 0.1875 mL 0.3749 mL 0.9373 mL
    20 mM 0.0281 mL 0.1406 mL 0.2812 mL 0.7030 mL
    25 mM 0.0225 mL 0.1125 mL 0.2250 mL 0.5624 mL
    30 mM 0.0187 mL 0.0937 mL 0.1875 mL 0.4687 mL
    40 mM 0.0141 mL 0.0703 mL 0.1406 mL 0.3515 mL
    50 mM 0.0112 mL 0.0562 mL 0.1125 mL 0.2812 mL
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます:C1V1 = C2V2

    濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
    × = ×
    C1   V1   C2   V2
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    • Do most proteins show cross-species activity?

      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.

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    製品名:
    RMC-5552
    製品番号:
    HY-132168
    数量:
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