1. Apoptosis
  2. MDM-2/p53
  3. RG7112

RG7112 (Synonyms: RO5045337)

Cat. No.: HY-10959 Purity: 99.91%
Handling Instructions

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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 231 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
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10 mg USD 252 In-stock
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25 mg USD 504 In-stock
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50 mg USD 768 In-stock
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100 mg USD 1128 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

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

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

    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.
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    • 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].

    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].

    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.

    939981-39-2

    SMILES

    C[[email protected]@]1([[email protected]](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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (137.40 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    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
    10 mM 0.1374 mL 0.6870 mL 1.3740 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.91%

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    Cat. No.:
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