1. Metabolic Enzyme/Protease
  2. Isocitrate Dehydrogenase (IDH)

Mutant IDH1 inhibitor 

Cat. No.: HY-13972 Purity: 98.03%
Handling Instructions

Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM.

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

Mutant IDH1 inhibitor Chemical Structure

Mutant IDH1 inhibitor Chemical Structure

CAS No. : 1429180-08-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 462 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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    Mutant IDH1 inhibitor purchased from MCE. Usage Cited in: Sci Rep. 2017 Oct 6;7(1):12758.

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

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM.

    IC50 & Target

    IC50: < 72 nM (mutant IDH1 R132H)

    In Vitro

    Mutant IDH1 inhibitor is a potent IDH1 R132H inhibitor, and used for the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer[1].

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 34 mg/mL (72.87 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1433 mL 10.7163 mL 21.4326 mL
    5 mM 0.4287 mL 2.1433 mL 4.2865 mL
    10 mM 0.2143 mL 1.0716 mL 2.1433 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Cell Assay
    [1]

    Day 1: cells are seeded in 384-well plates in triplicates for both the cell proliferation and 2HG assay, and incubated at 37°C, 95% Rh, 5% CO2 overnight. Day 2: compounds are serially diluted 1 :3 (10 point dilution from 10 mM solutions in DMSO) and delivered to the cell assay plates via acoustic dispenser, with final concentration ranging from 30 μM to 1.5 nM. The plates are returned to the incubator after treatment and incubated for 48 hours. Day 4 Proliferation assay: CTG is added to the assay plates and luminescence signal is read on the plate reader. Day 4 2HG assay : Extraction sample preparation consisted of aspirating all media from the assay plates, adding 70 μL of 90% methanol in water, dry ice incubation for 15 minutes, centrifuging at 2000 rpm for 30 min to ensure all particulates have settled, and transferring 30 μL of the supernatant into LC-MS ready plates. LC-MS analysis follows.

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

    References
    Molecular Weight

    466.58

    Formula

    C₂₅H₃₄N₆O₃

    CAS No.

    1429180-08-4

    SMILES

    CC(C)[[email protected]@H](COC1=O)N1C2=NC(N[[email protected]@H](C)C3=CC=C(CN4CCN(C(C)=O)CC4)C=C3)=NC=C2

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    × = ×
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    Product Name:
    Mutant IDH1 inhibitor
    Cat. No.:
    HY-13972
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    Mutant IDH1 inhibitor

    Cat. No.: HY-13972