2. Epigenetics
  3. Epigenetic Reader Domain
  4. MI-503

MI-503 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.

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

CAS No. : 1857417-13-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

MI-503 Related Antibodies

Top Publications Citing Use of Products

    MI-503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Jul 17;14(1):4259.  [Abstract]

    Western blot showing total and phosphorylated S6 in Farage and KARPAS422 (K422) cells with or without the treatment of MEN1 inhibitor (800 nM MI-503 for 3 days).

    MI-503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Feb 22;13(1):1006.  [Abstract]

    Quantitative real-time PCR analysis of Ptx3 in primary mESC treated with DMSO or MI-503(2 μM) in vitro.

    MI-503 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2021 Aug 26;40(1):270.  [Abstract]

    A significant decrease in colony formation in both AR-dependent and AR-independent PCa cells upon MI503 (2.5 μM) treatment by foci formation assays.

    MI-503 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2021 Aug 26;40(1):270.  [Abstract]

    Representative images of HE stained xenografts treated with DMSO (upper) and MI503 (75 mg/kg, i.p.).

    MI-503 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2021 Aug 26;40(1):270.  [Abstract]

    Representative images of IHC staining treated with MI503 (75 mg/kg, i.p.).

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    MI-503 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.

    Cellular Effect
    Cell Line Type Value Description References
    Bone marrow cell GI50
    0.22 μM
    Compound: 29; MI503
    Growth inhibition of MLL-AF9 transformed mouse bone marrow cells after 7 days by MTT assay
    Growth inhibition of MLL-AF9 transformed mouse bone marrow cells after 7 days by MTT assay
    		[PMID: 26744767]
    Bone marrow cell GI50
    > 5 μM
    Compound: 29; MI503
    Growth inhibition of Hoxa9/Meis1 transformed mouse bone marrow cells after 7 days by MTT assay
    Growth inhibition of Hoxa9/Meis1 transformed mouse bone marrow cells after 7 days by MTT assay
    		[PMID: 26744767]
    In Vitro

    MI-503 occupies the F9 and P13 pockets on menin, forming a hydrogen bond with Tyr276, and also extends beyond the P13 pocket to form hydrogen bonds with Trp341 and Glu366. Treatment of murine bone marrow cells (BMC) transformed with the mLL-AF9 oncogene with MI-503 results in substantial growth inhibition, with GI50 of 0.22 μM. The cell growth inhibitory effect of MI-503 is time-dependent, with a pronounced effect achieved after 7-10 days of treatment[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    MI-503 Related Antibodies
    In Vivo

    MI-503 achieves high level in peripheral blood following a single intravenous or oral dose, while also showing high oral bioavailability (75%). MI-503 induces strong inhibition of tumor growth with once daily intraperitoneal (i.p.) administration. Treatment with MI-503 results in an over 80% reduction in MV4;11 tumor volume and complete tumor regression in two mice. Ten consecutive days of treatment with MI-503 results in a marked delay in progression of mLL leukemia in mice and significantly reduces leukemia tumor burden. Treatment with MI-503 and MI-463 leads to markedly reduced expression of Hoxa9 and Meis1, downstream targets of mLL fusion proteins substantially upregulated in mLL leukemias[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    564.63

    Formula

    C28H27F3N8S
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    FC(F)(F)CC(S1)=CC2=C1N=CN=C2NC3CCN(CC4=CC=C(N(CC5=CNN=C5)C(C#N)=C6)C6=C4C)CC3
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (44.28 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 1.7711 mL 8.8554 mL 17.7107 mL
    5 mM 0.3542 mL 1.7711 mL 3.5421 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (3.68 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

      Solubility: ≥ 2.08 mg/mL (3.68 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  Corn Oil

      Solubility: 25 mg/mL (44.28 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  0.5% CMC/saline water

      Solubility: 25 mg/mL (44.28 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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).
    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

    Purity: 99.87%

    SDS (393 KB)

    COA (255 KB) LCMS (89 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    Leukemia cells are treated with MI-503 or 0.25% DMSO and cultured at 37 °C for 7 days. Media is changed at day 4, viable cell numbers are restored to the original concentration and MI-503 are re-supplied. MTT cell proliferation assay kit is then employed, and plates are read for absorbance at 570 nm using a microplate reader[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice: For efficacy studies in MV4;11 subcutaneous xenograft mice model, 5×106 cells are injected into the 4-6 week old female BALB/c nude mice. Treatment is started when the tumor size reached ~100 mm3. Vehicle (25% DMSO, 25% PEG400, 50% PBS) or compounds (MI-463 or MI-503) are administrated once daily at designated doses using i.p. injections[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7711 mL 8.8554 mL 17.7107 mL 44.2768 mL
    5 mM 0.3542 mL 1.7711 mL 3.5421 mL 8.8554 mL
    10 mM 0.1771 mL 0.8855 mL 1.7711 mL 4.4277 mL
    15 mM 0.1181 mL 0.5904 mL 1.1807 mL 2.9518 mL
    20 mM 0.0886 mL 0.4428 mL 0.8855 mL 2.2138 mL
    25 mM 0.0708 mL 0.3542 mL 0.7084 mL 1.7711 mL
    30 mM 0.0590 mL 0.2952 mL 0.5904 mL 1.4759 mL
    40 mM 0.0443 mL 0.2214 mL 0.4428 mL 1.1069 mL
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    MI-503 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-5031857417-13-0MI503MI 503Epigenetic Reader DomainInhibitorinhibitorinhibit

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