1. Apoptosis
  2. MDM-2/p53

RG7388 (Synonyms: Idasanutlin)

Cat. No.: HY-15676 Purity: 99.97% ee.: 99.55%
Handling Instructions

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

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

RG7388 Chemical Structure

RG7388 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 195 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 204 In-stock
Estimated Time of Arrival: December 31
50 mg USD 600 In-stock
Estimated Time of Arrival: December 31
100 mg USD 900 In-stock
Estimated Time of Arrival: December 31
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Customer Review

    RG7388 purchased from MCE. Usage Cited in: Haematologica. 2018 Jul 5. pii: haematol.2018.191650.

    Induction of tumor suppressor protein p53 in MV4-11 (A) and MOLM-13 cells (B) treated for 24 hours with the indicated amounts of NVP-HDM201 and midostaurin. Relative quantitation of CDKN1A mRNA (C) and MCL-1 mRNA (D) in AML cells treated for 24 hours with PKC412 and NVP-HDM201 alone or in combination.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

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

    IC50 & Target

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

    In Vitro

    RG7388 (Idasanutlin) 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]. RG7388 (300 nM or 1.8 μM) induces apoptosis in SJSA osteosarcoma cells[2].

    In Vivo

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

    Clinical Trial
    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.
    References
    Kinase Assay
    [1]

    The p53-MDM2 HTRF assay is performed in buffer containing 50 mM Tris-HCl, pH 7.4, 100 mM NaCl, 1 mM DTT, 0.02 or 0.2 mg/mL BSA. Small-molecule inhibitors are stored in aliquots as 10 mM stock solutions in DMSO at 4°C in 96-deep-well plates. It is thawed and mixed immediately prior to testing. The compound is incubated with GST-MDM2 and a biotinylated p53 peptide for one hour at 37°C. Phycolink goat anti-GST (Type 1) allophycocyanin and Eu-8044-streptavidin are then added and followed by one hour incubation at room temperature. Plates are read using the Envision fluorescence reader. IC50 values are determined from inter-plate duplicate or triplicate sets of data.

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

    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. 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
    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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.97% ee.: 99.55%

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    Product Name:
    RG7388
    Cat. No.:
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    Cat. No.: HY-15676