2234285-81-3
2234285-81-3 structure
- Name: IDH1 Inhibitor 1
- Chemical Name: IDH1 Inhibitor 1
- CAS Number: 2234285-81-3
- Molecular Formula: C20H18F4N6O2
- Molecular Weight: 450.39
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Isocitrate Dehydrogenase (IDH)
- Create Date: 2019-03-03 20:47:04
- Modify Date: 2024-01-04 12:59:59
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IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT, respectively[1]. Anticancer activity[1].
| Name | IDH1 Inhibitor 1 |
|---|
| Description | IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT, respectively[1]. Anticancer activity[1]. |
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| Related Catalog | |
| Target |
IC50: 0.021 μM (IDH1R132H), 0.045 μM (IDH1R132C), and 2.52 μM (IDH1WT)[1] |
| In Vitro | IDH1 Inhibitor 1 (Compound 19) inhibits cellular HCT116-IDH1R132H/+ with an IC50 of 0.039 μM[1]. |
| In Vivo | IDH1 Inhibitor 1 (Compound 19) inhibits 2-hydroxyglutarate (2-HG) production in a preclinical xenograft tumor model. 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[1]. |
| References |
| Molecular Formula | C20H18F4N6O2 |
|---|---|
| Molecular Weight | 450.39 |