TAS-121
Product Specifications
UNSPSC Description
TAS-121 is an orally active, selective, covalent, third-generation mutant EGFR-tyrosine kinase inhibitor (EGFR-TKI). TAS-121 inhibits the L858R mutation (IC50=1.7 nM), Ex19del mutation (IC50=2.7 nM), L858R/T790M mutation (IC50=0.56 nM) and Ex19del/T790M mutation (IC50=1.1 nM) and wild-type EGFR (IC50=8.2 nM). TAS-121 inhibits HER2 and HER4 with IC50s of 110 and 2.6 nM, respectively. TAS-121 inhibits phosphorylation of EGFR and its downstream signaling targets to block cell proliferation. TAS-121 induces apoptosis and displays antitumor activity in SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M) xenograft models[1].
Target Antigen
Apoptosis; EGFR
Type
Reference compound
Related Pathways
Apoptosis;JAK/STAT Signaling;Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/tas-121.html
Smiles
NC1=C2C(C3=CC4=C(C=CC=C4)N=C3)=C5N(C[C@H](CC5)NC(C=C)=O)C2=NC=N1
Molecular Weight
384.43
References & Citations
[1]Kimihiro Ito, et al. TAS-121, A Selective Mutant EGFR Inhibitor, Shows Activity Against Tumors Expressing Various EGFR Mutations Including T790M and Uncommon Mutations G719X. Mol Cancer Ther. 2019 May;18(5):920-928.
Shipping Conditions
Room temperature
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-164392/TAS-121-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-164392/
Clinical Information
No Development Reported
CAS Number
1451370-01-6
Curated Selection
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