Molecular Formula | C27H31FN4O2 |
Molar Mass | 462.56 |
Density | 1.21±0.1 g/cm3(Predicted) |
Boling Point | 707.6±60.0 °C(Predicted) |
Solubility | DMSO: soluble3mg/mL, clear |
Appearance | powder |
Color | white to beige |
pKa | 14.02±0.20(Predicted) |
Storage Condition | 2-8°C |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
In vitro study | AGI-5198 effective in inhibiting mutant IDH1(R132H-IDH1 and R132C-IDH1) but not wild-type IDH1 (IC50>100 μm) or any IDH2 subtype (R140Q, R172K, wild-type) (IC50>100 μm). AGI-5198 acts on TS603 glioma cell line, has anti-tumor effect, and inhibits R-2HG production, this effect is dose dependent. Under conditions of almost complete inhibition of R-2HG, AGI-5198 induced demethylation of histone H3K9me3 and induced gene expression associated with glial gene differentiation. In the whole genome DNA methylation, the growth of IDH1 mutant with impaired mIDH1 was inhibited, but there was no significant change in the growth of IDH1 wild type glioma cells. |
In vivo study | Treatment of AGI-5198 glioma xenografts at a dose of 450 mg/kg daily for three weeks on R132H-IDH1 inhibited growth by 50-60% and had no effect on the growth of IDH1 wild-type glioma xenografts. Tumor reduction in Ki-67 treated mice stained with AGI-5198 protein antibody. However, in the blank control group and the experimental group of AGI-5198 treated mice, there was no significant difference in the cleavage of caspase-3 in the tumor. |
Hazard Symbols | T - Toxic![]() |
Risk Codes | 25 - Toxic if swallowed |
Safety Description | 45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
UN IDs | UN 2811 6.1 / PGIII |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.162 ml | 10.809 ml | 21.619 ml |
5 mM | 0.432 ml | 2.162 ml | 4.324 ml |
10 mM | 0.216 ml | 1.081 ml | 2.162 ml |
5 mM | 0.043 ml | 0.216 ml | 0.432 ml |