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AdipoGen Life Sciences
AGI-5198
100
CHF
CHF 100.00
In stock
AG-CR1-3528-M0055 mgCHF 100.00
AG-CR1-3528-M02525 mgCHF 300.00
| Product Details | |
|---|---|
| Synonyms | N-[2-(Cyclohexylamino)-1-(2-methylphenyl)-2-oxoethyl]-N-(3-fluorophenyl)-2-methyl-1H-imidazole-1-acetamide; IDH-C35 |
| Product Type | Chemical |
| Properties | |
| Formula |
C27H31FN4O2 |
| MW | 462.6 |
| CAS | 1355326-35-0 |
| Purity Chemicals | ≥98% (NMR) |
| Appearance | White solid. |
| Solubility | Soluble in DMSO (10mg/ml) or ethanol (5mg/ml). |
| Identity | Determined by 1H-NMR. |
| InChi Key | FNYGWXSATBUBER-UHFFFAOYSA-N |
| Smiles | O=C(C(C1=C(C)C=CC=C1)N(C2=CC(F)=CC=C2)C(CN3C=CN=C3C)=O)NC4CCCCC4 |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Keep cool and dry. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- Potent and selective inhibitor of IDH1 (isocitrate dehydrogenase 1) R132H and R132C mutants in vitro with IC50 values of 0.07 and 0.16µM, respectively. Does not inhibit wild-type IDH1 or any of the examined IDH2 isoforms (IC50>100µM). Isocitrate dehydrogenases (IDHs) are nicotinamide adenine dinucleotide (NAD+) and NAD phosphate (NADP+)-dependent enzymes in the tricarboxylic acid (TCA) cycle that catalyze oxidative decarboxylation of isocitrate producing α-ketoglutarate (2-OG) and carbon dioxide. IDH1 and IDH2 are mutated in >70% of lower grade gliomas.
- Shown to have anti-tumor efficacy in the TS603 glioma cell line and to reduce tumor 2-HG production in HT1080 and U87MG cells.
- Caused 50-60% growth inhibition over a treatment period of three weeks with no affect in the growth of IDH1 wild-type glioma xenografts in R132H-IDH1 glioma xenografts.
- Under conditions of near complete 2-HG inhibition, induces demethylation of histone H3K9me3 and expression of genes associated with gliogenic differentiation.
- Useful chemical probe to assess the biological consequences of IDH1 mutations and the potential of IDH1 inhibition for treating IDH1 mutant tumors.
- Requires high doses for in vivo activity, but can be used through oral dosing route.
Product References
- Cancer-associated IDH1 mutations produce 2-hydroxyglutarate: L. Dang, et al.; Nature 462, 739 (2009)
- Transformation by the (R)-enantiomer of 2-hydroxyglutarate linked to EGLN activation: P. Koivunen, et al.; Nature 483, 484 (2012)
- IDH1 mutation is sufficient to establish the glioma hypermethylator phenotype: S. Turcan, et al., Nature 483, 479 (2012)
- Isocitrate dehydrogenase 1 and 2 mutations in cancer: alterations at a crossroads of cellular metabolism: Z.J. Reitman & H. Yan; J. Natl. Cancer Inst. 102, 932 (2010)
- Discovery of the first potent inhibitors of mutant IDH1 that lower tumor 2-HG in vivo: J. Popovici-Muller, et al.; ACS Med. Chem. Lett. 3, 850 (2012)
- An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells: D. Rohle, et al.; Science 340, 626 (2013)
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