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

Idasanutlin (Synonyms: RG7388)

Cat. No.: HY-15676 Purity: 99.90%
Handling Instructions

Idasanutlin (RG7388) is a potent and selective MDM2 antagonist, inhibiting p53-MDM2 binding, with an IC50 of 6 nM.

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

Idasanutlin Chemical Structure

Idasanutlin Chemical Structure

CAS No. : 1229705-06-9

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 95 In-stock
Estimated Time of Arrival: December 31
5 mg USD 70 In-stock
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10 mg USD 120 In-stock
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50 mg USD 290 In-stock
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100 mg USD 490 In-stock
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Customer Review

Based on 13 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Idasanutlin purchased from MCE. Usage Cited in: Preprints. 2018, 2018100121.

    Effect of SAHA and RG7388 treatments on Cell Cycle related Protein levels in MCF-7 cells. Figure shows upregulation of p21, p27, AURKB and CDC25C levels after treatment with 7.5 µM concentration of SAHA and p53 upregulation after RG7388 treatment.

    Idasanutlin purchased from MCE. Usage Cited in: Cells. 2018 Dec 22;8(1). pii: E8.

    Modulation of apoptosis-related protein expressions in MCF-7 cells after SAHA (7.5 μM), RG7388 (2.0 μM) and SAHA + RG7388 treatment for 24 h.

    Idasanutlin purchased from MCE. Usage Cited in: Cells. 2018 Dec 22;8(1). pii: E8.

    Modulation of necroptosis-related protein expressions in MCF-7 cells after (7.5 μM), RG7388 (2.0 μM) and SAHA + RG7388 treatment for 24 h

    Idasanutlin purchased from MCE. Usage Cited in: Cancer Res. 2019 May 1;79(9):2404-2414.

    Immunoblot for p53 pathway responses to 壹dasanutlin treatment (1 μM for 24h) in TTC642 cells reexpressing SMARCB1. Images are representative of three biological replicates.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Idasanutlin (RG7388) is a potent and selective MDM2 antagonist, inhibiting p53-MDM2 binding, with an IC50 of 6 nM.

    IC50 & Target

    IC50: 6 nM (p53-MDM2)[1]

    In Vitro

    Idasanutlin (RG7388) inhibits cell proliferation with IC50 of 30 nM, and induces dose-dependent p53 stabilization, cell cycle arrest, as well as cell apoptosis in cancer cells expressing wild-type p53[1]. Idasanutlin (RG7388) (300 nM or 1.8 μM) induces apoptosis in SJSA osteosarcoma cells[2].

    In Vivo

    Idasanutlin (RG7388, 25 mg/kg p.o.) results in tumor growth inhibition and regression, in the mouse SJSA human osteosarcoma xenograft model[1]. Idasanutlin (RG7388) induces induction of apoptosis and antiproliferation, in the SJSA xenograft model[2].

    Clinical Trial
    Molecular Weight

    616.48

    Formula

    C₃₁H₂₉Cl₂F₂N₃O₄

    CAS No.

    1229705-06-9

    SMILES

    O=C(O)C1=CC(OC)=C(NC([[email protected]]2[[email protected]](C3=C(F)C(Cl)=CC=C3)[[email protected]](C4=CC=C(Cl)C=C4F)(C#N)[[email protected]](CC(C)(C)C)N2)=O)C=C1

    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 : ≥ 45 mg/mL (73.00 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.6221 mL 8.1106 mL 16.2211 mL
    5 mM 0.3244 mL 1.6221 mL 3.2442 mL
    10 mM 0.1622 mL 0.8111 mL 1.6221 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: ≥ 2.5 mg/mL (4.06 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [1]

    Cell proliferation is evaluated by the tetrazolium dye assay. The concentration at which 50% inhibition (IC50) or 90% inhibition (IC90) of cell proliferation is determined from the linear regression of a plot of the logarithm of the concentration versus percent inhibition.

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

    Animal Administration
    [2]

    At 10 to 12 weeks of age, mice are implanted with a 1:1 mixture of human SJSA osteosarcoma cells (ATCC) suspended in phenol-free Matrigel and PBS. Mice are implanted in the right flank at a concentration of 5×106 cells in 0.2 mL total volume. At approximately day 10, animals are randomized according to tumor volume, so that all groups of 10 randomized mice have similar starting mean tumor volumes of 100 to 250 mm3. Idasanutlin (RG7388) is administered as an amorphous solid dispersion microbulk precipitate powder containing 30% drug substance and 70% hydroxypropyl methylcellulose acetate succinate polymer that is reconstituted immediately before administration as a suspension in Klucel/Tween, and remaining suspension is discarded after dosing.

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

    References

    Purity: 99.90%

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    KeyWords:

    Idasanutlin | RG7388 | RG 7388 | RG-7388 | MDM-2/p53 | Inhibitor | inhibitor | inhibit

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    Product name:
    Idasanutlin
    Cat. No.:
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