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AGI-5198

Cat. No. M2067
AGI-5198 Structure
Synonym:

IDH-C35

Size Price Availability Quantity
5mg USD 80 In stock
25mg USD 200 In stock
50mg USD 300 In stock
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Quality Control
Biological Activity

AGI-5198 (also know as IDH-C35) is a potent and selective mutant IDH1 inhibitor. AGI-5198 has been shown to have anti-tumor efficacy in the TS603 glioma cell line and to lower tumor 2-HG production in HT1080 and U87MG cells with IC50 values of 0.48 μM and 0.07 μM, respectively. AGI-5198 (IDH-C35) inhibits IDH1 R132H mutant and R132C mutant in vitro with IC50 of 0.07 μM and 0.16 μM respectively, but not wild-type IDH1 or any of the examined IDH2 isoforms (IC50 > 100 μM). In R132H-IDH1 glioma xenografts, AGI-5198 (450 mg/kg/day) caused 50-60% growth inhibition over a treatment period of three weeks with no affect in the growth of IDH1 wild-type glioma xenografts. Under conditions of near complete 2-HG inhibition, AGI-5198 can induce demethylation of histone H3K9me3 and expression of genes associated with gliogenic differentiation.

Customer Product Validations & Biological Datas
Source Cancer Res (2015). Figure 1. AGI-5198
Method Colony-forming assays
Cell Lines IDH1MT cells
Concentrations 800 nmol/L
Incubation Time 72 h
Results After 72 hours of incubation in the presence of AGI-5198, IDH-mediated NADPH production capacity of lDH1WT/R132H HCT116 cells was restored to levels comparable with those of lDH1WT/WT HCT116 cells
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 462.56
Formula C27H31FN4O2
CAS Number 1355326-35-0
Purity >99%
Solubility DMSO
Storage at -20°C
References

An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells.
Rohle D, et al. Science. 2013 May 3;340(6132):626-30. PMID: 23558169.

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Keywords: AGI-5198, IDH-C35 supplier, Dehydrogenase, inhibitors

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