TAS-121

Overview

TAS-121 is an orally active, selective, covalent, third-generation mutant EGFR-tyrosine kinase inhibitor (EGFR-TKI) . TAS-121 inhibits the L858R mutation ( IC 50 =1.7 nM), Ex19del mutation ( IC 50 =2.7 nM), L858R/T790M mutation ( IC 50 =0.56 nM) and Ex19del/T790M mutation ( IC 50 =1.1 nM) and wild-type EGFR ( IC 50 =8.2 nM). TAS-121 inhibits HER2 and HER4 with IC 50 s 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.

Application

Products | Products > Disease Areas > Cancer | Products > Signaling Pathways > JAK/STAT Signaling | Products > Signaling Pathways > Protein Tyrosine Kinase/RTK | Products > Signaling Pathways > Apoptosis | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Signaling Pathways > EGFR | Products > Signaling Pathways > Apoptosis

Product Information

• Catalog No.: HY-164392
• CAS No.: 1451370-01-6
• Molecular Formula: C22H20N6O
• Molecular Weight: 384.43
• Purity: 99.98%
• Storage: Please store the product under the recommended conditions in the Certificate of Analysis.

Source

Original product source