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IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1(R132) mutation with IC50 values of 27 nM, 28 nM and 6.14 μM for IDH1R132H, IDH1R132C and IDH1WT, respectively.
In vivo, IDH-305 (30-300 mg/kg; p.o.; twice daily for 21 days) inhibits 2-HG production and 2-HG-dependent tumor growth of an IDH1 mutant PDX melanoma model.
| Molecular Weight | 490.45 |
| Formula | C23H22F4N6O2 |
| CAS Number | 1628805-46-8 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Takeo Fujii, et al. Discov Med. Targeting isocitrate dehydrogenase (IDH) in cancer
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