1229705-06-9
Chemical Structure
Idasanutlin
Synonym(s): RG7388
- CAS No.: 1229705-06-9
- Formula:C31H29Cl2F2N3O4
- Molecular Weight:616.48
IUPAC Name: 4-((2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamido)-3-methoxybenzoic acid
InChIKey: TVTXCJFHQKSQQM-LJQIRTBHSA-N
SMILES: O=C(O)C1=CC(OC)=C(NC([C@H]2[C@H](C3=C(F)C(Cl)=CC=C3)[C@](C4=CC=C(Cl)C=C4F)(C#N)[C@H](CC(C)(C)C)N2)=O)C=C1
Biological Activity: Idasanutlin (RG7388) is an orally bioavailable MDM2 inhibitor with an IC50 of 6 nM. Idasanutlin disrupts MDM2-p53 binding, stabilizes and activates p53, triggering cell cycle arrest, apoptosis, and reduced cancer cell viability. Idasanutlin reduces EGFR protein expression and phosphorylation, suppresses downstream SHP2, MEK1/2, ERK1/2, AKT, mTOR, p70(S6K1), and S6 signaling. Idasanutlin induces mitochondrial ROS production, drives p38 MAPK phosphorylation, upregulates NOXA, and mediates caspase-3-dependent apoptosis and gasdermin E-mediated pyroptosis. Idasanutlin can be used for the research of TP53-mutant non-small cell lung cancer, T-cell acute lymphoblastic leukemia, colorectal carcinoma, melanoma, diffuse large B-cell lymphoma, mantle cell lymphoma, non-Hodgkin lymphoma, severe fever with thrombocytopenia syndrome, neuroblastoma, acute lymphoblastic leukemia, relapsed or refractory acute myeloid leukemia, osteosarcoma, solid tumors, and hematological tumors[1][2][3][4][5][6][7][8][9][10][11][12].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Idasanutlin | 99.93% | Idasanutlin (RG7388) is an orally bioavailable MDM2 inhibitor with an IC50 of 6 nM. Idasanutlin disrupts MDM2-p53 binding, stabilizes and activates p53, triggering cell cycle arrest, apoptosis, and reduced cancer cell viability. Idasanutlin reduces EGFR protein expression and phosphorylation, suppresses downstream SHP2, MEK1/2, ERK1/2, AKT, mTOR, p70(S6K1), and S6 signaling. Idasanutlin induces mitochondrial ROS production, drives p38 MAPK phosphorylation, upregulates NOXA, and mediates caspase-3-dependent apoptosis and gasdermin E-mediated pyroptosis. Idasanutlin can be used for the research of TP53-mutant non-small cell lung cancer, T-cell acute lymphoblastic leukemia, colorectal carcinoma, melanoma, diffuse large B-cell lymphoma, mantle cell lymphoma, non-Hodgkin lymphoma, severe fever with thrombocytopenia syndrome, neuroblastoma, acute lymphoblastic leukemia, relapsed or refractory acute myeloid leukemia, osteosarcoma, solid tumors, and hematological tumors. | ||||||||||||||||||||
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Idasanutlin (Standard) | ≥98% | Idasanutlin (Standard) is the analytical standard of Idasanutlin. This product is intended for research and analytical applications. Idasanutlin (RG7388) is a potent and selective MDM2 antagonist, inhibiting p53-MDM2 binding, with an IC50 of 6 nM. | ||||||||||||||||||||
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- [1]. Tang G, et al.. Repurposing MDM2 inhibitor RG7388 for TP53-mutant NSCLC: a p53-independent pyroptotic mechanism via ROS/p-p38/NOXA/caspase-3/GSDME axis. Cell death & disease. 2025 Jun 17;16(1):452. [Content Brief]
- [2]. Johansson KB, et al.. Idasanutlin and navitoclax induce synergistic apoptotic cell death in T-cell acute lymphoblastic leukemia. Leukemia. 2023 Dec;37(12):2356-2366. [Content Brief]
- [3]. Nieznanska A, et al.. Balancing cell cycle arrest and immune activation: A synergistic window for idasanutlin and anti-PD-1 therapy in a syngeneic mouse model. Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie. 2025 Dec;193:118868. [Content Brief]
- [4]. Herting F, et al. The triple combination of the CD20 antibody obinutuzumab with the Bcl-2 inhibitor venetoclax (GDC-199) and the MDM2 inhibitor idasanutlin results in superior efficacy and long term response in wildtype p53 NHL tumor models. Blood. 2016 Dec 2;128(22):4178.
- [5]. Liu Z, et al.. RG7388 inhibits SFTSV replication by suppressing MDM2-mediated p53 degradation and preventing apoptosome disruption. Science Bulletin. 2025 Jun 21. [Content Brief]
- [6]. Vernooij L, et al.. High-Throughput Screening Identifies Idasanutlin as a Resensitizing Drug for Venetoclax-Resistant Neuroblastoma Cells. Molecular cancer therapeutics. 2021 Jun;20(6):1161-1172. [Content Brief]
- [7]. Gu JJ, et al.. Targeting MDM2 and XIAP by Idasanutlin in diffuse large B-cell lymphoma. Blood. 2019 Nov 13;134:5301.
- [8]. Bell HL, et al. Preclinical investigation of the p53-MDM2 antagonist idasanutlin (RG7388) demonstrates significant activity in high risk adult acute lymphoblastic leukemia. Blood. 2020 Nov 5;136:38.
- [9]. Daver NG, et al.. Safety, efficacy, pharmacokinetic (PK) and biomarker analyses of BCL2 inhibitor venetoclax (Ven) plus MDM2 inhibitor idasanutlin (idasa) in patients (pts) with relapsed or refractory (R/R) AML: a phase Ib, non-randomized, open-label study. Blood. 2018 Nov 29;132:767.
- [10]. Ding Q, et al. Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. Journal of medicinal chemistry. 2013 Jul 25;56(14):5979-83. [Content Brief]
- [11]. Higgins B, et al. Preclinical optimization of MDM2 antagonist scheduling for cancer treatment by using a model-based approach. Clinical cancer research : an official journal of the American Association for Cancer Research. 2014 Jul 15;20(14):3742-52. [Content Brief]
- [12]. Lehmann C, et al.. Superior anti-tumor activity of the MDM2 antagonist idasanutlin and the Bcl-2 inhibitor venetoclax in p53 wild-type acute myeloid leukemia models. Journal of hematology & oncology. 2016 Jun 28;9(1):50. [Content Brief]
Keywords
