Formaat : 10mg
Synonyms:
| Description | mIDH1-IN-2 is a brain-penetrating inhibitor of isocitrate dehydrogenase 1 (IDH1). It demonstrates sub-nanomolar potency against IDH1R132H and R132C, with IC50 values of 80.0 and 58.0 nM, respectively, while showing minimal activity against wild-type IDH1/2. Additionally, mIDH1-IN-2 inhibits PDK1 with an IC50 of 0.61 μM and reduces phosphorylation levels of PDH in a dose-dependent manner. The compound also inhibits cell proliferation, induces S-phase arrest, and promotes apoptosis (apoptosis). mIDH1-IN-2 is applicable in cancer research, including studies on gliomas. |
| Targets & IC50 | R132H IDH1:80 nM |
| In vitro | mIDH1-IN-2 (Compound 27j) effectively inhibits the proliferation of HT1080 and U87-MG cells, with an EC50 value of 121.1 μM and 69.0 nM, respectively. Additionally, mIDH1-IN-2 at concentrations of 1-5 μM over 24-48 hours can induce S-phase arrest and apoptosis in U87-MG IDH1 R132H cells. |
| In vivo | Compound 27j, known as mIDH1-IN-2, is detectable in mouse brain tissue following intravenous injection. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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