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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.
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.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
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.
Keywords: Idasanutlin, Idasanutlin supplier, RG7388, MDM2, inhibitors, mdm2, p53, interaction, Ubiquitin, E3, Ligases, 6904, Tocris Bioscience
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:
There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.
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