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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)
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 |
| InChI Key | TVTXCJFHQKSQQM-LJQIRTBHSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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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Product Datasheets for Idasanutlin
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
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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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TPD and Induced Proximity Research Product GuideUpdated
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
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Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia