Pricing Availability   Qty
Description: Potent MDM2 inhibitor; inhibits MDM2-p53 interaction
Chemical Name: 4-[[[(2R,3S,4R,5S)-3-(3-Chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)-2-pyrrolidinyl]carbonyl]amino]-3-methoxybenzoic acid
Purity: ≥98% (HPLC)
Literature (3)

Biological Activity for Idasanutlin

Idasanutlin is a potent MDM2 inhibitor (IC50 = 6 nM in binding assay, and 30 nM in cancer cell proliferation assay). Induces p53 stabilisation, cell cycle arrest and apoptosis in cancer cells expressing wildtype p53. Displays inhibition of tumor growth in the SJSA1 tumor xenograft model. Also inhibits MDR-1 at high concentrations.

Compound Libraries for Idasanutlin

Idasanutlin is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for Idasanutlin

M. Wt 616.49
Formula C31H29Cl2F2N3O4
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1229705-06-9
PubChem ID 53358942
Smiles COC1=C(C=CC(C(O)=O)=C1)NC([C@@H]2N[C@H]([C@@]([C@H]2C3=C(C(Cl)=CC=C3)F)(C4=C(C=C(C=C4)Cl)F)C#N)CC(C)(C)C)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Idasanutlin

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 61.65 100

Preparing Stock Solutions for Idasanutlin

The following data is based on the product molecular weight 616.49. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.62 mL 8.11 mL 16.22 mL
5 mM 0.32 mL 1.62 mL 3.24 mL
10 mM 0.16 mL 0.81 mL 1.62 mL
50 mM 0.03 mL 0.16 mL 0.32 mL

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References for Idasanutlin

References are publications that support the biological activity of the product.

Ding et al (2013) Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. J.Med.Chem. 56 5979 PMID: 23808545

Chen et al (2014) Structurally diverse MDM2-p53 antagonists act as modulators of MDR-1 function in neuroblastoma. Br.J.Cancer. 111 716 PMID: 24921920

If you know of a relevant reference for Idasanutlin, please let us know.

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Keywords: Idasanutlin, Idasanutlin supplier, RG7388, MDM2, inhibitors, mdm2, p53, interaction, Ubiquitin, E3, Ligases, 6904, Tocris Bioscience

Citations for Idasanutlin

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Literature in this Area

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