TAS-121 is a selective, covalent third-generation mutant EGFR-tyrosine kinase inhibitor (EGFR-TKI) that targets various EGFR mutations, including L858R (IC50=1.7 nM), Ex19del (IC50=2.7 nM), L858R/T790M (IC50=0.56 nM), and Ex19del/T790M (IC50=1.1 nM), as well as wild-type EGFR (IC50=8.2 nM). It also exhibits inhibitory activity against HER2 and HER4 with IC50s of 110 and 2.6 nM, respectively. TAS-121 effectively inhibits EGFR phosphorylation and downstream signaling pathways, leading to reduced cell proliferation and induction of apoptosis. Its antitumor efficacy has been demonstrated in xenograft models utilizing SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M) cell lines.
TAS-121 is a selective, covalent third-generation mutant EGFR-tyrosine kinase inhibitor (EGFR-TKI) that targets various EGFR mutations, including L858R (IC50=1.7 nM), Ex19del (IC50=2.7 nM), L858R/T790M (IC50=0.56 nM), and Ex19del/T790M (IC50=1.1 nM), as well as wild-type EGFR (IC50=8.2 nM). It also exhibits inhibitory activity against HER2 and HER4 with IC50s of 110 and 2.6 nM, respectively. TAS-121 effectively inhibits EGFR phosphorylation and downstream signaling pathways, leading to reduced cell proliferation and induction of apoptosis. Its antitumor efficacy has been demonstrated in xenograft models utilizing SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M) cell lines.
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