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IDH1 Inhibitor 1 is an orally bioavailable, brain-penetrant, and selective mutant IDH1 inhibitor (IC50s: 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $1,970 | 10-14 weeks | 10-14 weeks | |
| 50 mg | $2,580 | 10-14 weeks | 10-14 weeks | |
| 100 mg | $3,400 | 10-14 weeks | 10-14 weeks |
| Description | IDH1 Inhibitor 1 is an orally bioavailable, brain-penetrant, and selective mutant IDH1 inhibitor (IC50s: 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT). |
| Targets&IC50 | IDH1 (WT):2.52 μM , IDH1 (R132H):0.021 μM , IDH1 (R132C):0.045 μM |
| In vitro | IDH1 Inhibitor 1 inhibits cellular HCT116-IDH1R132H/+ with an IC50 of 0.039 μM. |
| In vivo | IDH1 Inhibitor 1 is also profiled in a patient-derived IDH1 mutant HCT116-IDH1R132H/+ mechanistic xenograft tumor model in mice to evaluate in vivo inhibition of 2-HG production. IDH1 Inhibitor 1, dosed orally at 150 mg/kg, inhibits new 2-HG production.IDH1 Inhibitor 1 ?inhibits 2-hydroxyglutarate (2-HG) production in a preclinical xenograft tumor model. |
| Molecular Weight | 450.39 |
| Formula | C20H18F4N6O2 |
| Cas No. | 2234285-81-3 |
| Smiles | C[C@H](Nc1nccc(n1)N1[C@@H](CF)COC1=O)c1cn(cn1)-c1ccc(cc1)C(F)(F)F |
| Relative Density. | 1.31g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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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