IDH1 Inhibitor 1

Modify Date: 2024-01-04 12:59:59

IDH1 Inhibitor 1 Structure
IDH1 Inhibitor 1 structure
Common Name IDH1 Inhibitor 1
CAS Number 2234285-81-3 Molecular Weight 450.39
Density N/A Boiling Point N/A
Molecular Formula C20H18F4N6O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of IDH1 Inhibitor 1


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].

 Names

Name IDH1 Inhibitor 1

 IDH1 Inhibitor 1 Biological Activity

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].
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

[1]. Zhao Q, et al. Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Orally Bioavailable and Brain Penetrant Mutant IDH1 Inhibitors. ACS Med Chem Lett. 2018 Jun 11;9(7):746-751.

 Chemical & Physical Properties

Molecular Formula C20H18F4N6O2
Molecular Weight 450.39