TC-E 5008

Pricing Availability   Qty
Cat.No. 5244 - TC-E 5008 | C13H13NO2 | CAS No. 50405-58-8
Description: Selective mutant isocitrate dehydrogenase 1 (mIDH1) inhibitor; phenotypically lethal
Alternative Names: SYC 435
Chemical Name: 1-Hydroxy-4-methyl-6-(phenylmethyl)-2-(1H)pyridinone
Datasheet
Citations
Reviews
Literature

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

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.

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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

References

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


If you know of a relevant reference for TC-E 5008, please let us know.

View Related Products by Target

View Related Products by Product Action

View all Isocitrate Dehydrogenase 1 (IDH1) Inhibitors

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

Citations for TC-E 5008

Citations are publications that use Tocris products.

Currently there are no citations for TC-E 5008. Do you know of a great paper that uses TC-E 5008 from Tocris? Please let us know.

Reviews for TC-E 5008

There are currently no reviews for this product. Be the first to review TC-E 5008 and earn rewards!

Have you used TC-E 5008?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Epigenetics

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

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

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.