Idasanutlin | p53-MDM2 inhibitor

Idasanutlin (1229705-06-9) is a potent (IC₅₀ = 6 nM) and selective inhibitor of MDM2, the primary negative regulator of p53.¹ It blocks the p53-MDM2 interaction activating the p53 pathway leading to cell cycle arrest and apoptosis.  Idasanutlin has displayed efficacy in the treatment of multiple cancers alone and in combination with other chemotherapeutics.^2-6

References/Citations:

1. Ding et al. (2013), Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development; J. Med. Chem. 56 5979
2. Cui et al. (2020), Combination of metformin and RG7388 enhances inhibition of growth and induction of apoptosis of ovarian cancer cells through the PI3K/AKT/mTOR pathway; Biochem. Biophys. Res. Commun. 533 665
3. Vernooij et al. (2021), High-Throughput Screening Identifies Idasanutlin as a Resinsitizing Drug for Venetoclax-Resistant Neuroblastoma Cells; Mol. Cancer Ther. 20 1161
4. Wang et al. (2022), Genome-wide CROSPR/Cas9 screening for therapeutic targets in NSCLC carrying wild-type TP53 and receptor tyrosine kinase genes; Clin. Transl. Med. 12 e882
5. Johansson et al. (2023), Idasanutlin and navitoclax induce synergistic apoptotic cell death in T-cell acute Lymphoblastic leukemia; Leukemia 37 2356
6. Neubauer et al. (2025), Pharmacological Inhibition of MDM2 Induces Apoptosis in p53-Mutated Triple-Negative Breast Cancer; Int. J. Mol. Sci. 26 1078