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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
IDH1
Curated Selection
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