[CAS NO. 1355326-35-0] AGI-5198
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PRODUCTS SPECIFICATIONS [1355326-35-0]
Store
Catalog
SLK-S7185
Brand
Selleck
CAS
1355326-35-0
DESCRIPTION [1355326-35-0]
Overview
| MDL | MFCD24848688 |
|---|---|
| Molecular Weight | 462.56 |
| Molecular Formula | C27H31FN4O2 |
| SMILES | O=C(NC1CCCCC1)C(N(C2=CC=CC(F)=C2)C(CN3C=CN=C3C)=O)C4=CC=CC=C4C |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1619 mL | 10.8094 mL | 21.6188 mL |
| 5 mM | 0.4324 mL | 2.1619 mL | 4.3238 mL |
| 10 mM | 0.2162 mL | 1.0809 mL | 2.1619 mL |
| 50 mM | 0.0432 mL | 0.2162 mL | 0.4324 mL |
Description
AGI-5198 (IDH-C35) is the first highly potent and selective inhibitor of mutants with of 0.07 μM/0.16 μM.
In vitro
AGI-5198, potently inhibits mutant IDH1 (R132H-IDH1 and R132C-IDH1), but not wildtype IDH1 (IC50 > 100 μM) or any of IDH2 isoforms (R140Q, R172K, wildtype) (IC50 > 100 μM). AGI-5198, has been shown to have anti-tumor efficacy in the TS603 glioma cell line and to block R-2HG production in a dose-dependent manner. Under conditions of near-complete R-2HG inhibition, AGI-5198 induced demethylation of histone H3K9me3 and expression of genes associated with gliogenic differentiation. Blockade of mIDH1 impaired the growth of IDH1-mutant—but not IDH1–wild-type—glioma cells without appreciable changes in genome-wide DNA methylation.
In vivo
In R132H-IDH1 glioma xenografts, AGI-5198 (450 mg/kg/day) causes 50-60% growth inhibition over a treatment period of three weeks with no affect in the growth of IDH1 wild-type glioma xenografts. Tumors from AGI-5198-treated mice shows reduced staining with an antibody against the Ki-67 protein. But cleaved caspase-3 shows no differences between tumors from vehicle and AGI-5198–treated mice.
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