IDH889 is a potent and selective inhibitors of IDH1. IDH899 shows IDH (R132H) IC50 = 20 nM; Cell 2-HG IC50 = 14 nM. IDH889 demonstrates significantly improved plasma exposure in mice vs IDH662 (AUC 3.6 μM·h, Cmax 1.7 μM at 10 mg/kg; AUC 55.5 μM·h, Cmax 14.2 μM at 100 mg/kg). IDH889 also has excellent permeability and no efflux in the Caco-2 and human MDR1-MDCK cell lines, supporting the hypothesis that potent inhibition of mutant IDH1 function by binding at the allosteric binding site is compatible with brain penetration.
MedKoo Cat#: 406991
Name: IDH889
CAS#: 1429179-07-6
Chemical Formula: C23H25FN6O2
Exact Mass: 436.2023
Molecular Weight: 436.49
Elemental Analysis: C, 63.29; H, 5.77; F, 4.35; N, 19.25; O, 7.33
The following data is based on the product molecular weight 436.49 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
