TAS6417 (Synonyms: TAS6417; CLN-081) |
| Catalog No.GC32752 |
TAS6417(CLN-081)은 1.1-8.0 nM 범위의 IC50 값으로 EGFR 힌지 영역의 ATP 결합 부위에 고유한 스캐폴드 피팅이 있는 매우 효과적인 경구 활성 및 범 돌연변이 선택적 EGFR 티로신 키나제 억제제입니다.
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Cas No.: 1661854-97-2
Sample solution is provided at 25 µL, 10mM.
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TAS6417 is an EGFR inhibitor and an efficacious drug candidate for patients with NSCLC, with IC50 values ranging from 1.1-8.0 nM.
TAS6417 inhibits the in vitro phosphorylation activity of EGFR and its mutants including an exon 20 insertion mutation, with IC50 values ranging from 1.1±0.1 to 8.0±1.1 nM. TAS6417 suppresses the growth of cells expressing exon 20 insertion mutations of the EGFR gene, with a GI50 value of 86.5±28.5 nM for LXF 2478L cells and 45.4±2.6 nM for NCI-H1975 EGFR D770_N771insSVD cells. TAS6417 also potently inhibits proliferation in other cell lines harboring activating mutations or acquired resistance mutations, with mean GI50 values of 1.92±0.21 nM to 7.12±0.60 nM. In contrast, the effect of TAS6417 on cell proliferation in normal human epidermal keratinocytes (NHEK-Neo), of which WT EGFR is implicates in the growth and survival, is moderate[1].
TAS6417 causes persistent tumor regression in vivo in EGFR exon 20 insertion-driven tumor models. TAS6417 inhibits mutant EGFR in tumors but not WT EGFR in skin tissues. TAS6417 prolongs survival of animals bearing lung cancer[1].
[1]. Hasako S, et al. TAS6417, A Novel EGFR Inhibitor Targeting Exon 20 Insertion Mutations. Mol Cancer Ther. 2018 Aug;17(8):1648-1658.
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