TC-E 5008

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Cat.No. 5244 - TC-E 5008 | C13H13NO2 | CAS No. 50405-58-8
Description: Selective mutant isocitrate dehydrogenase 1 (mIDH1) inhibitor; phenotypically lethal
Chemical Name: 1-Hydroxy-4-methyl-6-(phenylmethyl)-2-(1H)pyridinone
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Biological Activity

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.

Technical Data

M. Wt 215.25
Formula C13H13NO2
Storage Store at +4°C
CAS Number 50405-58-8
PubChem ID 13590964
InChI Key AVLZAVSZOAQKRC-UHFFFAOYSA-N
Smiles O=C1C=C(C)C=C(CC2=CC=CC=C2)N1O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 21.52 100
ethanol 21.52 100

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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

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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

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References

References are publications that support the products' biological activity.

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-E5008 selective mutant isocitrate dehydrogenase 1 (IDH1) inhibitors inhibits phenotypically lethal cancer gliomas D-2-hydroxyglutaric acid Other Dehydrogenases

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