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Selective mutant isocitrate dehydrogenase 1 (mIDH1) inhibitor (Ki = 120-190 nM). Displays >60-fold selectivity for mIDH1 (found in ~75% of gliomas) over wild type IDH1. Also inhibits D-2-hydroxyglutaric acid in cells expressing mIDH1 (EC50 = 2.4 μM). Does not display cytotoxicity towards non-cancerous human cells. Phenotypically lethal.
|Storage||Store at +4°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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 215.25. 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|
|1 mM||4.65 mL||23.23 mL||46.46 mL|
|5 mM||0.93 mL||4.65 mL||9.29 mL|
|10 mM||0.46 mL||2.32 mL||4.65 mL|
|50 mM||0.09 mL||0.46 mL||0.93 mL|
References are publications that support the biological activity of the product.
Zheng et al (2013) Crystallographic investigation and selective inhibition of mutant isocitrate dehydrogenase. ACS Med.Chem.Lett. 4 542 PMID: 23795241
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Keywords: TC-E 5008, TC-E 5008 supplier, TC-E5008, selective, mutant, isocitrate, dehydrogenase, 1, (IDH1), inhibitors, inhibits, phenotypically, lethal, cancer, gliomas, D-2-hydroxyglutaric, acid, SYC435, SYC, 435, Isocitrate, 5244, Tocris Bioscience
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Cancer Metabolism Poster
Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the main targets for cancer metabolism researchers. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways. These distinct metabolic circuits could provide viable cancer therapeutic targets.
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.