TAS-121

• 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

• Clinical Information:

  No Development Reported

• CAS Number:

  1451370-01-6