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Idasanutlin

Catalog No. T6254   CAS 1229705-06-9
Synonyms: RG7388, Ro 5503781

Idasanutlin (Ro 5503781) (RG-7388) is an effective and specific p53-MDM2 inhibitor (IC50: 6 nM).

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Idasanutlin Chemical Structure
Idasanutlin, CAS 1229705-06-9
Pack Size Availability Price/USD Quantity
2 mg In stock $ 34.00
5 mg In stock $ 55.00
10 mg In stock $ 97.00
25 mg In stock $ 162.00
50 mg In stock $ 238.00
100 mg In stock $ 396.00
500 mg In stock $ 929.00
1 mL * 10 mM (in DMSO) In stock $ 76.00
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Purity: 99.55%
Purity: 99.13%
Purity: 99.01%
Purity: 98.85%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Idasanutlin (Ro 5503781) (RG-7388) is an effective and specific p53-MDM2 inhibitor (IC50: 6 nM).
Targets&IC50 MDM2:6 nM
In vitro 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]
In vivo In a mouse SJSA human osteosarcoma xenograft model, Idasanutlin (25 mg/kg p.o.) causes tumor growth inhibition and regression. [1] In a SJSA xenograft model, Idasanutlin results in induction of apoptosis and antiproliferation. [2]
Kinase Assay Biochemical Binding Affinity – HTRF Assay: 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. Data are analyzed by XLfit4 (Microsoft) using a 4 Parameter Logistic Model (Sigmoidal Dose-Response Model) and the equation Y= (A+ ((B-A)/ (1+ ((C/x)^D)))), where A and B are enzyme activity in the absence or presence of infinite inhibitor compound, respectively, C is the IC50 and D is the Hill coefficient.
Cell Research 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. (Only for Reference)
Synonyms RG7388, Ro 5503781
Molecular Weight 616.48
Formula C31H29Cl2F2N3O4
CAS No. 1229705-06-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 93 mg/mL (150.9 mM)

Ethanol: 8 mg/mL (12.97 mM), Heating is recommended.

TargetMolReferences and Literature

1. Ding Q, et al. J Med Chem. 2013, 56(14), 5979-5983. 2. Higgins B, et al. Clin Cancer Res. 2014, 20(14), 3742-3752.

TargetMolCitations

1. Vollmer J, Ecker J, Hielscher T, et al.Class I HDAC inhibition reduces DNA damage repair capacity of MYC-amplified medulloblastoma cells.Journal of Neuro-Oncology.2023: 1-16.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Fluorochemical Library Stem Cell Differentiation Compound Library Autophagy Compound Library Anti-Cancer Compound Library Pyroptosis Compound Library

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Keywords

Idasanutlin 1229705-06-9 Apoptosis Ubiquitination E1/E2/E3 Enzyme Mdm2 E3 ligating enzyme inhibit Ubiquitin activating enzyme RG-7388 E2 conjugating enzyme E1 activating enzyme Ubiquitin conjugating enzyme MDM-2/p53 RG 7388 Inhibitor RG7388 Ubiquitin ligase Ro 5503781 inhibitor

 

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