2. Apoptosis Metabolic Enzyme/Protease
  3. MDM-2/p53 E1/E2/E3 Enzyme
  4. RG7112

RG7112 is a potent, selective, first clinical, orally active and blood-brain barrier crossed MDM2-p53 inhibitor, with an IC50 of 18 nM and a KD of 11 nM for binding to MDM2.

For research use only. We do not sell to patients.

RG7112 Chemical Structure

RG7112 Chemical Structure

CAS No. : 939981-39-2

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 192 In-stock
Solution
10 mM * 1 mL in DMSO USD 192 In-stock
Solid
5 mg USD 120 In-stock
10 mg USD 210 In-stock
25 mg USD 420 In-stock
50 mg USD 640 In-stock
100 mg USD 950 In-stock
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Customer Review

Based on 16 publication(s) in Google Scholar

RG7112 Related Antibodies

Top Publications Citing Use of Products

    RG7112 purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2016 Mar 1;22(5):1185-96.  [Abstract]

    p53, p21 and MDM2 protein levels in MDM2-amplified GBM line treated with RG7112.

    RG7112 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Nov 15;7(46):75328-75338.  [Abstract]

    Cell viability and activation of TP53 target proteins in clear cell carcinomas treated with RG7112. A and B. Time- (A) and dose-dependent (B) accumulation of MDM2, TP53, and TP21, as measured by western blotting. RG7112 is added at 2.5 μM in (A). C. Induction of TP53 phosphorylation and TP53 target proteins (TP21 and PUMA), as determined by western blotting. Cleaved PARP and survivin are also assessed to detect proapoptotic signaling.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    RG7112 is a potent, selective, first clinical, orally active and blood-brain barrier crossed MDM2-p53 inhibitor, with an IC50 of 18 nM and a KD of 11 nM for binding to MDM2[1].

    IC50 & Target

    Kd: 11 nM (MDM2)[1]
    In Vitro

    RG7112 (0-5 μM) stabilizes wild-type p53 and induces p53 signaling in cancer cells. RG7112 effectively activates p53 functions in cancer cells[1][2].

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

    RG7112 Related Antibodies

    Cell Proliferation Assay[2]

    Cell Line: SJSA1 osteosarcoma cells.
    Concentration: 0-5 μM.
    Incubation Time: 0-60 hours.
    Result: Dose-dependently inhibited the growth and killed SJSA1 osteosarcoma cells expressing high levels of MDM2 protein due to MDM2 gene amplification.

    Cell Cycle Analysis[2]

    Cell Line: HCT116 and SJSA1 cells.
    Concentration: 0-5 μM.
    Incubation Time: 48 hours.
    Result: Induced a dose-dependent cell cycle block in G1 and G2/M phase and depletion of the S phase compartment.
    In Vivo

    RG7112 (25-200 mg/kg, single oral dose) activates p53 pathway and induces apoptosis in tumor cells in vivo[2].
    ? RG7112 (100 mg/kg, gavage once per day, 5 days/week for 3 weeks ) reduces tumor growth rate and increases survival in GBM models[3].

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

    Animal Model: Female Balb/c nude mice[2].
    Dosage: 25-200 mg/kg.
    Administration: Orally, single dose.
    Result: At the highest dose level of RG7112 (200 mg/kg) only 1.2% (± 0.89 SD) of cells incorporated BrdU at 24 h post-dosing, vs. 14% (± 1.83 SD) of vehicle treated tumors.
    Animal Model: GBM cells were implanted into the brain of Athymic Nude mice (7 weeks old females, 10 animals/group)[3].
    Dosage: 100 mg/kg.
    Administration: Oral gavage, once per day, 5 days/week for 3 weeks.
    Result: Reduced tumor growth rate and increases survival in heterotopic and orthotopic animal models bearing MDM2-amplified GBM.
    Clinical Trial
    Molecular Weight

    727.78

    Formula

    C38H48Cl2N4O4S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    C[C@@]1([C@](C)(N(C(C2=CC=C(C=C2OCC)C(C)(C)C)=N1)C(N3CCN(CC3)CCCS(=O)(C)=O)=O)C4=CC=C(C=C4)Cl)C5=CC=C(C=C5)Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 200 mg/mL (274.81 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 1.3740 mL 6.8702 mL 13.7404 mL
    5 mM 0.2748 mL 1.3740 mL 2.7481 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration
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    Volume
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    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: ≥ 10 mg/mL (13.74 mM); Clear solution

      This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 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: ≥ 10 mg/mL (13.74 mM); Clear solution

      This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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.
    Purity & Documentation

    Purity: 99.91%

    COA (259 KB) HNMR (196 KB) LCMS (450 KB)

    Handling Instructions (2659 KB)
    References

    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 1.3740 mL 6.8702 mL 13.7404 mL 34.3510 mL
    5 mM 0.2748 mL 1.3740 mL 2.7481 mL 6.8702 mL
    10 mM 0.1374 mL 0.6870 mL 1.3740 mL 3.4351 mL
    15 mM 0.0916 mL 0.4580 mL 0.9160 mL 2.2901 mL
    20 mM 0.0687 mL 0.3435 mL 0.6870 mL 1.7176 mL
    25 mM 0.0550 mL 0.2748 mL 0.5496 mL 1.3740 mL
    30 mM 0.0458 mL 0.2290 mL 0.4580 mL 1.1450 mL
    40 mM 0.0344 mL 0.1718 mL 0.3435 mL 0.8588 mL
    50 mM 0.0275 mL 0.1374 mL 0.2748 mL 0.6870 mL
    60 mM 0.0229 mL 0.1145 mL 0.2290 mL 0.5725 mL
    80 mM 0.0172 mL 0.0859 mL 0.1718 mL 0.4294 mL
    100 mM 0.0137 mL 0.0687 mL 0.1374 mL 0.3435 mL
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    RG7112 Related Classifications

    Help & FAQs
    • 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.

    Keywords:

    RG7112939981-39-2RO5045337RG 7112RG-7112RO 5045337RO-5045337MDM-2/p53E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseInhibitorinhibitorinhibit

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