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Cat. No. Name Size Price Add Cart
KI2122AGI-519810 mg$430
AGI-519825 mg$1072

Chemical Characteristic

Product NameAGI-5198
SynonymsN/A
CAS No.1355326-35-0
Molecular Weight 462.56
FormulaC27H31FN4O2
Chemical Namen-(2-(cyclohexylamino)-1-(2-methylphenyl)-2-oxoethyl)-n-(3-fluorophenyl)-2-methyl-1h-imidazole-1-acetamide
SmilesC(=O)(C(c1c(cccc1)C)N(C(=O)Cn1c(ncc1)C)c1cc(ccc1)F)NC1CCCCC1
Chemical Structure

Biological activities

AGI-5198 is a potent and selective inhibitor of IDH1 R132H and R132C mutants. The IC50s of AGI-5198 against IDH1 R132H and R132C mutants are 70 and 160 nM, respectively. However, the IC50s of AGI-5198 against wild-type IDH1, wild-type IDH2, or IDH2 mutants are > 100 μM.[1] In vitro, AGI-5198 inhibits tumor 2-HG production in HT1080 and U87MG cells with IC50s of 480 and 70 nM, respectively. In vivo, AGI-5198 administration shows robust tumor 2-HG inhibition in U87 R132H mouse xenograft model.[2] AGI-5198 administration (450 mg/kg) shows 50-60% growth inhibition in R132H-IDH1 glioma xenografts, while has no affect in the growth of IDH1 wild-type glioma xenografts.[1]

Protocols

In vivo: AGI-5198 is dissolved in 0.5% MC and 0.2% Tween 80.[1]

References

[1] Rohle D, et al. An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells. Science. 2013, 340(6132): 626-630.
[2] Janeta Popovici-Muller, et al. Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG in Vivo. ACS Med Chem Lett. 2012, 3(10): 850-855.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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