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AGI-5198

CAS No. : 1355326-35-0

MCE 站：AGI-5198

产品活性：AGI-5198 (IDH-C35) 是有效和选择性的突变体 IDH1^R132H 抑制剂，IC₅₀ 为 0.07 μM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Isocitrate Dehydrogenase (IDH)

In Vitro: Measurements of R-2HG concentrations in pellets of TS603 glioma cells demonstrates dose-dependent inhibition of the mutant IDH1 enzyme by AGI-5198. AGI-5198 does not impair colony formation of two patient-derived glioma lines that express only the wild-type IDH1 allele (TS676 and TS516). Cancer cells heterozygous for the IDH1(R132H) mutation exhibits less IDH-mediated production of NADPH, such that after exposure to ionizing radiation (IR), there are higher levels of reactive oxygen species, DNA double-strand breaks, and cell death compared with IDH1 wild-type cells. These effects are reversed by the IDH1(R132H) inhibitor AGI-5198.

In Vivo: AGI-5198 (450 mg/kg, p.o.) causes 50 to 60% growth inhibition of the tumor growth from human glioma xenografts. Tumors from AGI-5198- treated mice show reduced staining with an antibody against the Ki-67 protein. AGI-5198 does not affect the growth of IDH1 wild-type glioma xenografts.

相关产品：Bioactive Compound Library Plus  |  Metabolism/Protease Compound Library  |  Anti-Cancer Compound Library  |  Glutamine Metabolism Compound Library  |  GSK864  |  Mutant IDH1-IN-1  |  Mutant IDH1-IN-2  |  IDH1 Inhibitor 1  |  Mutant IDH1-IN-4

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