bis-Imidazole phenol is a potent and cell permeable inhibitor of isocitrate dehydrogenase 1 (IDH1) mutant R132H that inhibits D-2-hydroxyglutaric acid (2HG) production in cells. bis-Imidazole phenol binds to an IDH1 R132H allosteric site at the dimer interface containing residue involved in binding of the catalytically essential divalent cation.
| Molecular Weight | 366.5 |
| Formula | C22H30N4O |
| CAS Number | 1648909-73-2 |
| Solubility (25°C) | DMSO: 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Isocitrate Dehydrogenase (IDH) Products |
|---|
| 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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