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

MI-773 TFA is an orally active, selective MDM2-p53 interaction inhibitor with a Ki of 0.88 nM for MDM2. MI-773 TFA blocks the MDM2-TP53 interaction. MI-773 TFA potently activates p53. MI-773 TFA induces Apoptosis. MI-773 TFA causes tumor regression in xenograft models of adenoid cystic carcinoma. MI-773 TFA exhibits anticancer effects in neuroblastoma. MI-773 TFA can be used for the research of adenoid cystic carcinoma.

For research use only. We do not sell to patients.

CAS No. : 1303609-37-1

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of MI-773 TFA:

MI-773 TFA Related Antibodies

Top Publications Citing Use of Products

    MI-773 TFA 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.

    • Biological Activity

    • Purity & Documentation

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    • Customer Review

    Description

    MI-773 TFA is an orally active, selective MDM2-p53 interaction inhibitor with a Ki of 0.88 nM for MDM2. MI-773 TFA blocks the MDM2-TP53 interaction. MI-773 TFA potently activates p53. MI-773 TFA induces Apoptosis. MI-773 TFA causes tumor regression in xenograft models of adenoid cystic carcinoma. MI-773 TFA exhibits anticancer effects in neuroblastoma. MI-773 TFA can be used for the research of adenoid cystic carcinoma[1][2].

    In Vivo

    MI-773 (10-100 mg/kg; p.o.; daily) TFA 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) TFA mediates significant tumor regression in the ACCx6 adenoid cystic carcinoma PDX model[1].
    MI-773 (100 mg/kg; p.o.; daily) TFA 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.
    Molecular Weight

    676.53

    Formula

    C31H35Cl2F4N3O5
    CAS No.
    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.OC(C(F)(F)F)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (147.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.4781 mL 7.3907 mL 14.7813 mL
    5 mM 0.2956 mL 1.4781 mL 2.9563 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 (sealed storage, away from moisture). 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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    In Vivo:

    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    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (3.70 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (3.70 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    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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    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 (sealed storage, away from moisture)

    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.
    Purity & Documentation
    References

    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 (sealed storage, away from moisture). 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 1.4781 mL 7.3907 mL 14.7813 mL 36.9533 mL
    5 mM 0.2956 mL 1.4781 mL 2.9563 mL 7.3907 mL
    10 mM 0.1478 mL 0.7391 mL 1.4781 mL 3.6953 mL
    15 mM 0.0985 mL 0.4927 mL 0.9854 mL 2.4636 mL
    20 mM 0.0739 mL 0.3695 mL 0.7391 mL 1.8477 mL
    25 mM 0.0591 mL 0.2956 mL 0.5913 mL 1.4781 mL
    30 mM 0.0493 mL 0.2464 mL 0.4927 mL 1.2318 mL
    40 mM 0.0370 mL 0.1848 mL 0.3695 mL 0.9238 mL
    50 mM 0.0296 mL 0.1478 mL 0.2956 mL 0.7391 mL
    60 mM 0.0246 mL 0.1232 mL 0.2464 mL 0.6159 mL
    80 mM 0.0185 mL 0.0924 mL 0.1848 mL 0.4619 mL
    100 mM 0.0148 mL 0.0739 mL 0.1478 mL 0.3695 mL
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    MI-773 TFA Related Classifications

    Help & FAQs
    • 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-7731303609-37-1MI773MI 773MDM-2/p53Apoptosisp21G2/M phase checkpoint genesG1 cell cycle arrestMDM2-p53 interactionp53apoptosisMDM2patient-derived xenograft modelsadenoid cystic carcinomaneuroblastoma cellsInhibitorinhibitorinhibit

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