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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 |
[3] Takeo Fujii, et al. Discov Med. Targeting isocitrate dehydrogenase (IDH) in cancer
| Related Isocitrate Dehydrogenase (IDH) Products |
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| Mutant IDH1-IN-4
Mutant IDH1-IN-4 is an inhibitor of mutant isocitrate dehydrogenase 1 (IDH 1) with an IC50 value of ≤ 0.5 μM for mutant IDH 1 in R132H, HT1080 and U87R132H cells. |
| (S,S)-GSK321
(S,S)-GSK321 is the (S,S)-enantiomer of GSK321.GSK321 is a potent inhibitor of the mutant isocitrate dehydrogenase 1 (IDH1) enzyme. |
| IDH1 Inhibitor 1
IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-permeable, selective mutant IDH1 inhibitor that inhibits IDH1R132H, IDH1R132C, and IDH1WT with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM, respectively. possesses antitumor activity. |
| IDH1 Inhibitor 7
IDH1 Inhibitor 7 is an IDH1 inhibitor with an IC50 of less than 100 nM. |
| (R,R)-GSK321
(R,R)-GSK321 is an isomer of GSK321 and a wild-type isocitrate dehydrogenase 1 (WT IDH1) inhibitor with an IC50 value of 120 nM. |
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