2. Apoptosis
  3. MDM-2/p53 Apoptosis
  4. MI-773

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.

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CAS 番号 : 1303607-07-9

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 193 在庫あり
Solution
10 mM * 1 mL in DMSO USD 193 在庫あり
Solid
5 mg $156 在庫あり
10 mg $252 在庫あり
25 mg $529 在庫あり
50 mg $972 在庫あり
100 mg $1800 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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カスタマーレビュー

Based on 6 publication(s) in Google Scholar

Other Forms of MI-773:

MI-773 関連抗体

Top Publications Citing Use of Products

    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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    • 純度とドキュメンテーション

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    製品説明

    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[1][2].

    体内実験

    MI-773 (10-100 mg/kg; p.o.; daily) induces dose-dependent tumor growth inhibition and regression in the UM-PDX-HACC-5 adenoid cystic carcinoma model, with 100 mg/kg mediating a 127% TGI index and 86% tumor shrinkage via p53-dependent apoptosis[1].
    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.

    Animal Model: CB.17.SCID (male and female, severe combined immunodeficient)[1]
    Dosage: 10 mg/kg; 50 mg/kg; 100 mg/kg
    Administration: p.o.; daily
    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.
    分子量

    562.50

    分子式

    C29H34Cl2FN3O3
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    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
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
    溶剤 & 溶解度
    体外: 

    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.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7778 mL 8.8889 mL 17.7778 mL
    5 mM 0.3556 mL 1.7778 mL 3.5556 mL
    10 mM 0.1778 mL 0.8889 mL 1.7778 mL
    View the 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.

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    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.

    • Protocol 1

      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.
    • Protocol 2

      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.
    In Vivo Dissolution Calculator
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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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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: 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)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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
    参考文献

    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
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    MI-773 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    MI-7731303607-07-9MI773MI 773MDM-2/p53ApoptosisInhibitorinhibitorinhibit

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    製品名:
    MI-773
    製品番号:
    HY-17493
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