Idasanutlin-d3-1
Based on 1 Customer Validation
Idasanutlin-d3-1 (RG7388-d3-1) is the deuterated-labeled Idasanutlin (HY-15676). 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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 99.57%
- 화학식: C31H26D3Cl2F2N3O4
- 분자량:619.50
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
IC50 & Target
IC50: 6 nM (p53-MDM2)[1]
In Vitro
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
신청
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Unlabeled CAS 1229705-22-9
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Appearance Solid
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분자량 619.50
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화학식 C31H26D3Cl2F2N3O4
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Color White to off-white
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SMILES
O=C(NC1=C(OC([2H])([2H])[2H])C=C(C(O)=O)C=C1)[C@H](N[C@H]2CC(C)(C)C)[C@H](C3=CC=CC(Cl)=C3F)[C@@]2(C#N)C4=CC=C(Cl)C=C4F
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Synonyms
RG7388-d3-1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 100 mg/mL (161.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (284 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[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]
[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]
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6142 mL | 8.0710 mL | 16.1421 mL | 40.3551 mL |
| 5 mM | 0.3228 mL | 1.6142 mL | 3.2284 mL | 8.0710 mL | |
| 10 mM | 0.1614 mL | 0.8071 mL | 1.6142 mL | 4.0355 mL | |
| 15 mM | 0.1076 mL | 0.5381 mL | 1.0761 mL | 2.6903 mL | |
| 20 mM | 0.0807 mL | 0.4036 mL | 0.8071 mL | 2.0178 mL | |
| 25 mM | 0.0646 mL | 0.3228 mL | 0.6457 mL | 1.6142 mL | |
| 30 mM | 0.0538 mL | 0.2690 mL | 0.5381 mL | 1.3452 mL | |
| 40 mM | 0.0404 mL | 0.2018 mL | 0.4036 mL | 1.0089 mL | |
| 50 mM | 0.0323 mL | 0.1614 mL | 0.3228 mL | 0.8071 mL | |
| 60 mM | 0.0269 mL | 0.1345 mL | 0.2690 mL | 0.6726 mL | |
| 80 mM | 0.0202 mL | 0.1009 mL | 0.2018 mL | 0.5044 mL | |
| 100 mM | 0.0161 mL | 0.0807 mL | 0.1614 mL | 0.4036 mL |
Idasanutlin-d3-1 Related Classifications
HY-153939S Related Classifications
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Keywords
- Idasanutlin-d3-1
- RG7388-d3-1
- Isotope-Labeled Compounds
- MDM-2/p53
- E1/E2/E3 Enzyme
- Apoptosis
- Pyroptosis
- Reactive Oxygen Species (ROS)
- Caspase
- non-small cell lung cancer
- diffuse large B-cell lymphoma
- severe fever with thrombocytopenia syndrome virus
- neuroblastoma
- acute myeloid leukemia
- MDM2
- T-cell acute lymphoblastic leukemia
- p53
- colorectal carcinoma
- melanoma
- Inhibitor
- inhibitor
- inhibit