TC-E 5008

TC-E 5008 is a potent mutant IDH1 inhibitor with Ki values of 190 nM and 120 nM for R132H and R132C IDH1 mutants, respectively. TC-E 5008 exhibits very weak activity against WT-IDH1 with a Ki value of 12.3 μM. TC-E 5008 has anti-proliferative activity on multiple ER positive breast cancer cell lines[1][2].

Product Specifications

CAS Number

[50405-58-8]

UNSPSC

12352005

Target

Isocitrate Dehydrogenase (IDH)

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/tc-e-5008.html

Solubility

10 mM in DMSO

Smiles

ON1C(CC2=CC=CC=C2)=CC(C)=CC1=O

Molecular Formula

C13H13NO2

Molecular Weight

215.25

References & Citations

[1]Baisong Zheng, et al. Crystallographic Investigation and Selective Inhibition of Mutant Isocitrate Dehydrogenase. ACS Med Chem Lett. 2013 Jun 13;4 (6) :542-546.|[2]Vasanth S. Murali, et al. Cancer drug discovery as a low rank tensor completion problem. bioRxiv, March 9, 2021.