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Biological Activity for AGI 5198
AGI 5198 is a potent and selective inhibitor of mutant isocitrate dehydrogenase 1 (mIDH1; IC50 = 70 nM). Selective for mIDH1 over wild-type IDH1 and IDH2. Inhibits production of oncometabolite D-2 hydroxyglutarate. Attenuates growth of glioma cells containing mIDH1, but not wild-type IDH1, in vitro and in vivo. Also inhibits growth of fibrosarcoma and chondrosarcoma cells bearing mIDH1.
Compound Libraries for AGI 5198
Technical Data for AGI 5198
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for AGI 5198
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for AGI 5198
The following data is based on the product molecular weight 462.56. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||4.32 mL||21.62 mL||43.24 mL|
|2.5 mM||0.86 mL||4.32 mL||8.65 mL|
|5 mM||0.43 mL||2.16 mL||4.32 mL|
|25 mM||0.09 mL||0.43 mL||0.86 mL|
References for AGI 5198
References are publications that support the biological activity of the product.
Rohle et al (2013) An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells. Science 340 626 PMID: 23558169
Li et al (2015) Treatment with a small molecule mutant IDH1 inhibitor suppresses tumorigenic activity and decreases production of the oncometabolite 2-hydroxyglutarate in human chondrosarcoma cells. PLoS ONE 10 e0133813 PMID: 26368816
Badur et al (2018) Oncogenic R132 IDH1 mutations limit NADPH for de novo lipogenesis through (D)2-hydroxyglutarate production in fibrosarcoma cells. Cell Rep. 25 1018 PMID: 30355481
If you know of a relevant reference for AGI 5198, please let us know.
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Citations for AGI 5198
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