MI-773
Based on 6 publication(s) in Google Scholar
MI-773 is an orally active, selective MDM2-p53 interaction inhibitor with a Ki of 0.88 nM for MDM2. MI-773 blocks the MDM2-TP53 interaction. MI-773 potently activates p53. MI-773 induces Apoptosis. MI-773 causes tumor regression in xenograft models of adenoid cystic carcinoma. MI-773 exhibits anticancer effects in neuroblastoma. MI-773 TFA can be used for the research of adenoid cystic carcinoma.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 96.29%
- CAS 番号: 1303607-07-9
- 分子式: C29H34Cl2FN3O3
- 分子量:562.50
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保管条件:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 MI-773
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生物活性
MI-773 (100 mg/kg; p.o.; daily) mediates significant tumor regression in the ACCx6 adenoid cystic carcinoma PDX model[1].
MI-773 (100 mg/kg; p.o.; daily) mediates significant tumor regression in the ACCx9 adenoid cystic carcinoma PDX model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB.17.SCID (male and female, severe combined immunodeficient)[1]
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Dosage:10 mg/kg; 50 mg/kg; 100 mg/kg
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Administration:p.o.; daily
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Result:Modestly reduced tumor growth rate, resulting in a tumor growth inhibition (TGI) index of 34% and final average tumor volume of 600 mm3 at 20 days of treatment (10 mg/kg).
Caused significant tumor regression, with a TGI index of 127%, 86% tumor shrinkage, and final average tumor volume of 30 mm3 at 20 days of treatment (100 mg/kg).
Increased time to tumor failure (defined as 2x increase in pre-treatment volume; p=0.044) (100 mg/kg).
Increased percentage of TUNEL-positive apoptotic cells (p=0.015) and p53-positive cells (p<0.001) in tumor tissue, with p53 localization shifted from nuclear to cytoplasmic (100 mg/kg).
Increased p53 and phospho-p53 (Ser392) protein levels in tumor lysates (50 or 100 mg/kg).
Showed no observable weight loss in all treatment groups.
化学情報
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CAS 番号 1303607-07-9
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性状 Solid
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分子量 562.50
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分子式 C29H34Cl2FN3O3
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Color White to off-white
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SMILES
O=C([C@H](N[C@@H]1CC(C)(C)C)[C@H](C2=CC=CC(Cl)=C2F)[C@]31C(NC4=C3C=CC(Cl)=C4)=O)N[C@H]5CC[C@H](O)CC5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (6)
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Journal Impact Factor
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Most Recent
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Nat Chem Biol
Discovery and characterization of highly potent and selective allosteric USP7 inhibitors. [Abstract]2018 Feb;14(2):118-125. PMID: 29200206
MI-773 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2018 Feb;14(2):118-125. [Abstract]
HCT 116 cells are treated with 4, ent-4 and SAR405838 for 2 h and lysed for western blotting analysis probing for USP7, p53, p-Ser15-p53, p21, MDM2 and β-actin as indicated.
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Cells
PROTAC-Mediated Targeted Degradation of MDM2 Induces Tumor-Suppressive Signaling in Osteosarcoma Cells. [Abstract]2026 Mar 5;15(5):473. PMID: 41827906 -
Int J Mol Sci
Improving Reporter Gene Assay Methodology for Evaluating the Ability of Compounds to Restore P53 Activity. [Abstract]2022 Nov 10;23(22):13867. PMID: 36430341 -
BMC Biol
A yeast two-hybrid system for the screening and characterization of small-molecule inhibitors of protein-protein interactions identifies a novel putative Mdm2-binding site in p53. [Abstract]2017 Nov 9;15(1):108. PMID: 29121928 -
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Mater Sci Eng C Mater Biol Appl
A stimuli-responsive combination therapy for recovering p53-inactivation associated drug resistance. [Abstract]2020 Mar;108:110403. PMID: 31923941
溶剤 & 溶解度
DMSO : ≥ 53 mg/mL (94.22 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (stored under nitrogen). 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (281 KB)
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- English - EN (393 KB)
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- Korean - KR (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Zhang Q, et al. Targeting p53-MDM2-MDMX loop for cancer therapy. Subcell Biochem. 2014;85:281-319. [Content Brief]
[2]. Tatyana A Grigoreva, et al. Amino acids as chiral derivatizing agents for antiproliferative substituted N-benzyl isoindolinones. Chirality. 2018 Jun;30(6):785-797. [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 (stored under nitrogen). 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 | 1.7778 mL | 8.8889 mL | 17.7778 mL | 44.4444 mL |
| 5 mM | 0.3556 mL | 1.7778 mL | 3.5556 mL | 8.8889 mL | |
| 10 mM | 0.1778 mL | 0.8889 mL | 1.7778 mL | 4.4444 mL | |
| 15 mM | 0.1185 mL | 0.5926 mL | 1.1852 mL | 2.9630 mL | |
| 20 mM | 0.0889 mL | 0.4444 mL | 0.8889 mL | 2.2222 mL | |
| 25 mM | 0.0711 mL | 0.3556 mL | 0.7111 mL | 1.7778 mL | |
| 30 mM | 0.0593 mL | 0.2963 mL | 0.5926 mL | 1.4815 mL | |
| 40 mM | 0.0444 mL | 0.2222 mL | 0.4444 mL | 1.1111 mL | |
| 50 mM | 0.0356 mL | 0.1778 mL | 0.3556 mL | 0.8889 mL | |
| 60 mM | 0.0296 mL | 0.1481 mL | 0.2963 mL | 0.7407 mL | |
| 80 mM | 0.0222 mL | 0.1111 mL | 0.2222 mL | 0.5556 mL |
MI-773 関連分類
HY-17493 関連分類
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