1. Apoptosis
  2. MDM-2/p53

RG7388 (Synonyms: Idasanutlin)

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

RG7388 is a potent and selective p53-MDM2 antagonist 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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $163 In-stock
5 mg $120 In-stock
10 mg $170 In-stock
50 mg $500 In-stock
100 mg $750 In-stock
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500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

IC50: 6 nM (p53-MDM2)

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].

References
Preparing Stock Solutions
Concentration Volume 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.
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]

RG7388 is prepared in 30% drug substance and 70% hydroxypropyl methylcellulose acetate succinate polymer.

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

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

Solvent & Solubility

DMSO: ≥ 45 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.97% ee.: 99.55%

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