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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C31H29Cl2F2N3O4 |
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分子量 | 616.48 | CAS No. | 1229705-06-9 | ||||
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (162.21 mM) | ||||
Water | Insoluble | ||||||
Ethanol | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Idasanutlin (RG7388) is a potent and selective p53-MDM2 inhibitor with IC50 of 6 nM showing improved in vitro binding as well as cellular potency/selectivity. |
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in vitro | Idasanutlin inhibits cell proliferation with IC50 of 30 nM, and induces dose-dependent p53 stabilization, cell cycle arrest, as well as cell apoptosis in cancer cells expressing wild-type p53. [1] |
in vivo | In a mouse SJSA human osteosarcoma xenograft model, Idasanutlin (25 mg/kg p.o.) causes tumor growth inhibition and regression. [1] In a SJSA xenograft model, Idasanutlin results in induction of apoptosis and antiproliferation. [2] |
キナーゼアッセイ | Biochemical Binding Affinity – HTRF Assay | |
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The p53-MDM2 HTRF assay is performed in buffer containing 50 mM Tris-HCl, pH 7.4, 100 mM NaCl, 1 mM DTT, 0.02 or 0.2 mg/ml BSA. Small-molecule inhibitors are stored in aliquots as 10 mM stock solutions in DMSO at 4°C in 96-deep-well plates. It is thawed and mixed immediately prior to testing. The compound is incubated with GST-MDM2 and a biotinylated p53 peptide for one hour at 37°C. Phycolink goat anti-GST (Type 1) allophycocyanin and Eu-8044-streptavidin are then added and followed by one hour incubation at room temperature. Plates are read using the Envision fluorescence reader. IC50 values are determined from inter-plate duplicate or triplicate sets of data. Data are analyzed by XLfit4 (Microsoft) using a 4 Parameter Logistic Model (Sigmoidal Dose-Response Model) and the equation Y= (A+ ((B-A)/ (1+ ((C/x)^D)))), where A and B are enzyme activity in the absence or presence of infinite inhibitor compound, respectively, C is the IC50 and D is the Hill coefficient. | ||
細胞アッセイ | 細胞株 | wt-p53 cancer cell lines (SJSA1, RKO, HCT116) |
濃度 | ~10 μM | |
反応時間 | 24 hours | |
実験の流れ | Cell proliferation is evaluated by the tetrazolium dye assay. The concentration at which 50% inhibition (IC50) or 90% inhibition (IC90) of cell proliferation is determined from the linear regression of a plot of the logarithm of the concentration versus percent inhibition. |
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動物実験 | 動物モデル | Mice bearing SJSA human osteosarcoma xenografts |
投薬量 | ~50 mg/kg daily | |
投与方法 | p.o. |
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Adipocyte p53 coordinates the response to intermittent fasting by regulating adipose tissue immune cell landscape [ Nat Commun, 2024, 15(1):1391] | PubMed: 38360943 |
miR-16-5p enhances sensitivity to RG7388 through targeting PPM1D expression (WIP1) in Childhood Acute Lymphoblastic Leukemia [ Cancer Drug Resist, 2023, 6(2):242-256] | PubMed: 37457129 |
Genome-wide CRISPR/Cas9 screening for therapeutic targets in NSCLC carrying wild-type TP53 and receptor tyrosine kinase genes [ Clin Transl Med, 2022, 12(6):e882] | PubMed: 35692096 |
Epstein Barr virus-positive B-cell lymphoma is highly vulnerable to MDM2 inhibitors in vivo [ Blood Adv, 2022, 6(3):891-901] | PubMed: 34861697 |
FOXO1 Is a Key Mediator of Glucocorticoid-Induced Expression of Tristetraprolin in MDA-MB-231 Breast Cancer Cells [ Int J Mol Sci, 2022, 23(22)13673] | PubMed: 36430156 |
Novel MDM2 Inhibitor XR-2 Exerts Potent Anti-Tumor Efficacy and Overcomes Enzalutamide Resistance in Prostate Cancer [ Front Pharmacol, 2022, 13:871259] | PubMed: 35548335 |
p53 Regulates a miRNA-Fructose Transporter Axis in Brown Adipose Tissue Under Fasting [ Front Genet, 2022, 13:913030] | PubMed: 35734423 |
Negative value of CD10-/CD34- immunophenotype in pediatric leukemia and development of a related cell line model for investigating drug resistance [ Clin Transl Oncol, 2022, 10.1007/s12094-021-02755-x] | PubMed: 34985639 |
Suppression of HSF1 activity by wildtype p53 creates a driving force for p53 loss-of-heterozygosity [ Nat Commun, 2021, 12(1):4019] | PubMed: 34188043 |
Epstein Barr virus-positive B-cell lymphoma is highly vulnerable to MDM2 inhibitors in vivo [ Blood Adv, 2021, bloodadvances.2021006156] | PubMed: 34861697 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。