1. Metabolic Enzyme/Protease
  2. Isocitrate Dehydrogenase (IDH)
  3. Mutant IDH1-IN-2

Mutant IDH1-IN-2 is a inhibitor of mutant Isocitrate dehydrogenase (IDH) proteins, with IC50 of in LS-MS biochemical assay, IC50 of 16.

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

Mutant IDH1-IN-2 Chemical Structure

Mutant IDH1-IN-2 Chemical Structure

CAS No. : 1429176-69-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 303 In-stock
Solution
10 mM * 1 mL in DMSO USD 303 In-stock
Solid
5 mg USD 300 In-stock
10 mg USD 500 In-stock
25 mg USD 950 In-stock
50 mg USD 1550 In-stock
100 mg   Get quote  
200 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products
WB

    Mutant IDH1-IN-2 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Oct 6;7(1):12758.  [Abstract]

    Represented western blot of an isothermal dose-response at melting temperature of 59°C demonstrating cellular mIDH1 enzyme thermal stabilization with mIDH1 inhibitors.

    View All Isocitrate Dehydrogenase (IDH) Isoform Specific Products:

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Mutant IDH1-IN-2 is a inhibitor of mutant Isocitrate dehydrogenase (IDH) proteins, with IC50 of in LS-MS biochemical assay, IC50 of 16.6 nM in Fluorescence biochemical assay. Target: Mutant IDH1 Mutant IDH1-IN-2 has a neomorphic activity and in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer. More bioactivity information in Patent WO 2013046136A1 (Example 224).

    IC50 & Target

    IDH1

     

    Molecular Weight

    459.53

    Formula

    C24H31F2N5O2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1OC[C@H](C(C)C)N1C2=NC(N[C@H](C3=CC=C(CN4CCC(F)(F)CC4)C=C3)C)=NC=C2

    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 : 50 mg/mL (108.81 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 2.1761 mL 10.8807 mL 21.7614 mL
    5 mM 0.4352 mL 2.1761 mL 4.3523 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    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.44 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:

    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: 98.50%

    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 2.1761 mL 10.8807 mL 21.7614 mL 54.4034 mL
    5 mM 0.4352 mL 2.1761 mL 4.3523 mL 10.8807 mL
    10 mM 0.2176 mL 1.0881 mL 2.1761 mL 5.4403 mL
    15 mM 0.1451 mL 0.7254 mL 1.4508 mL 3.6269 mL
    20 mM 0.1088 mL 0.5440 mL 1.0881 mL 2.7202 mL
    25 mM 0.0870 mL 0.4352 mL 0.8705 mL 2.1761 mL
    30 mM 0.0725 mL 0.3627 mL 0.7254 mL 1.8134 mL
    40 mM 0.0544 mL 0.2720 mL 0.5440 mL 1.3601 mL
    50 mM 0.0435 mL 0.2176 mL 0.4352 mL 1.0881 mL
    60 mM 0.0363 mL 0.1813 mL 0.3627 mL 0.9067 mL
    80 mM 0.0272 mL 0.1360 mL 0.2720 mL 0.6800 mL
    100 mM 0.0218 mL 0.1088 mL 0.2176 mL 0.5440 mL
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    Mutant IDH1-IN-2 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.

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    Product Name:
    Mutant IDH1-IN-2
    Cat. No.:
    HY-18717
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