AGI 5198

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Cat.No. 7087 - AGI 5198 | C27H31FN4O2 | CAS No. 1355326-35-0
Description: Potent and selective inhibitor of mutant isocitrate dehydrogenase 1 (mIDH1)
Chemical Name: N-[2-(Cyclohexylamino)-1-(2-methylphenyl)-2-oxoethyl]-N-(3-fluorophenyl)-2-methyl-1H-Imidazole-1-acetamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

Biological Activity

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.

Technical Data

M. Wt 462.56
Formula C27H31FN4O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1355326-35-0
PubChem ID 56645356
InChI Key FNYGWXSATBUBER-UHFFFAOYSA-N
Smiles CC1=NC=CN1CC(=O)N(C(C(=O)NC1CCCCC1)C1=C(C)C=CC=C1)C1=CC(F)=CC=C1

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 23.13 50
ethanol 4.63 10

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
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

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References

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


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Keywords: AGI 5198, AGI 5198 supplier, AGI5198, potent, selective, inhibitor, inhibits, mutant, isocitrate, dehydrogenase, 1, mIDH1, oncometabolites, D-2, hydroxyglutarate, D-2HG, Isocitrate, (IDH1), 7087, Tocris Bioscience

Citations for AGI 5198

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Literature in this Area

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Cancer

Cancer Research Product Guide

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Epigenetics Scientific Review

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Cancer Metabolism Poster

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Epigenetics in Cancer Poster

Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.