| Identification | Back Directory | [Name]
2-Propenamide, N-[(8S)-4-amino-6,7,8,9-tetrahydro-5-(3-quinolinyl)pyrimido[5,4-b]indolizin-8-yl]- | [CAS]
1451370-01-6 | [Synonyms]
2-Propenamide, N-[(8S)-4-amino-6,7,8,9-tetrahydro-5-(3-quinolinyl)pyrimido[5,4-b]indolizin-8-yl]- | [Molecular Formula]
C22H20N6O | [MOL File]
1451370-01-6.mol | [Molecular Weight]
384.43 |
| Hazard Information | Back Directory | [Uses]
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]. | [IC 50]
EGFR L858R: 1.7 nM (IC50); EGFR (ex19del): 2.7 nM (IC50); EGFR L858R/T790M: 0.56 nM (IC50); EGFR (ex19del/T790M): 1.1 nM (IC50); EGFR (WT): 8.2 nM (IC50); HER2: 110 nM (IC50); HER4: 2.6 nM (IC50) | [References]
[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. DOI:10.1158/1535-7163.MCT-18-0645 |
|
|