Idasanutlin
CAS No.: 1229705-06-9
Purity: >98%
HNMR
Idasanutlin is a potent and selective MDM2 ligand widely utilized in PROTAC research and targeted protein degradation studies. As an "E3 Ligase Ligand," Idasanutlin binds specifically to the MDM2 E3 ubiquitin ligase, enabling the recruitment of MDM2 to target proteins for ubiquitination and subsequent proteasomal degradation. This mechanism is central to the PROTAC (Proteolysis Targeting Chimera) technology, which leverages bifunctional molecules to induce the selective elimination of disease-causing proteins. Idasanutlin-based conjugates are extensively used to design and optimize MDM2-mediated PROTACs, providing valuable tools for oncology and therapeutics research targeting proteins such as p53 regulators. Its high affinity and specificity make it an essential building block in the development of revolutionary protein degradation drugs and chemical probes in the field of targeted therapy.
Structure of 1229705-06-9
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* For research and manufacturing use only. Not for human or clinical use.
| Size | Price | Stock | Quantity |
|---|---|---|---|
| 200 mg | $399 | In stock |
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Background Introduction
Idasanutlin is a potent, selective, small-molecule antagonist of the Murine Double Minute 2 (MDM2) protein. As part of the Nutlin family, Idasanutlin inhibits the MDM2-p53 protein-protein interaction, leading to reactivation of the p53 tumor suppressor pathway. Given its robust binding affinity and high selectivity, Idasanutlin is widely studied in oncology and increasingly leveraged in the design of innovative PROTAC molecules targeting the MDM2 E3 ligase system.
Mechanism
Idasanutlin functions by directly binding the p53-binding pocket on the MDM2 E3 ubiquitin ligase, thereby preventing the degradation of p53 mediated by MDM2. In a PROTAC context, Idasanutlin serves as a ligand for MDM2, recruiting this E3 ligase to the target protein of interest when linked via an appropriate chemical linker. This proximity enables ubiquitination of the target protein, leading to its selective proteasomal degradation. The use of Idasanutlin in PROTAC design facilitates the development of bifunctional molecules capable of modulating protein levels with high specificity.
Applications
Idasanutlin is widely used in the research and development of MDM2-based PROTACs, providing a viable E3 ligase recruitment strategy for targeted protein degradation. Its primary applications include:
• Design of bifunctional degraders for challenging or undruggable targets using MDM2 recruitment• Mechanistic studies on p53 pathway modulation and E3 ligase-mediated TPD (targeted protein degradation)
• Screening platforms and drug discovery efforts focused on oncology and related therapeutic areas
• Optimization and SAR (structure-activity relationship) studies of MDM2 ligands as part of degrader and molecular glue libraries
Idasanutlin's robust performance and versatility make it a valuable tool for PROTAC research, chemical biology, and targeted therapeutics innovation.
• Consistent batch-to-batch reproducibility with complete QC documentation
• Supplied with COA, MSDS, and analytical data for traceability
• Reliable global shipping with stability-guaranteed packaging
• Dedicated technical support and optional custom synthesis service
• Demonstrates strong binding affinity to CRBN, VHL, or other E3 ligases
• Enables stable E3 ligase recruitment for targeted protein degradation
• Selective MDM2 inhibitor, making it an optimal warhead for PROTAC development targeting the p53-MDM2 interaction.
• High potency and well-characterized pharmacological profile facilitate efficient design of cancer-targeted therapeutics.
| ConcentrationVolumeMass | 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 |
| 50 mM | 0.0324 mL | 0.1622 mL | 0.3244 mL |
Hello, please give information about the mechanism by which Idasanutlin damages tumor cells.
OK!Idasanutlin through blocking p53−MDM2 binding and effectively activates the p53 pathway, leading to cell cycle arrest and/or apoptosis in cell lines expressing wild-type p53 and tumor growth inhibition or regression of osteosarcoma xenografts in nude mice.
16/1/2016
Hi! May I know the current research status of Idasanutlin?
Yes! It is currently in three phase I clinical trials for treatment of patients with solid tumors, acute myelogenous leukemia, or advanced malignancies as a single agent and in combination with chemotherapeutics.
14/3/2020
Hi! please describe the PK properties about Idasanutlin.Thanks.
No thanks! In mice, it has oral bioavailability (80%), moderate clearance (t1/2 = 1.6 h).
30/3/2020
activates the p53 pathway
Idasanutlin blocks p53–MDM2 binding and effectively activates the p53 pathway.It worked as expected.
24/8/2018
MDM2 inhibitor
Used in our lab, no complaints, worked well. all the characteristics expected of an MDM2 inhibitor in terms of specific binding to the target, mechanistic outcomes resulting from activation of the p53 pathway, and in vivo efficacy.
10/1/2019
tumor growth inhibition
Recommend everyone to use. Idasanutlin shows tumor growth inhibition and regression of osteosarcoma xenografts in nude mice.
18/4/2020
* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2
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