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DC12161  (CAS:1661854-97-2)
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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.
CAS Number: 1661854-97-2


Molecular Weight: 396.44
Molecular Formula: C23H20N6O
Quality Control: HPLCNMR LC/MS(Please contact us to get the QC report)
Synonyms: TAS-6417,TAS 6417,TAS6417
Chemical Name:
Storage: 2 years -20C Powder, 2 weeks4C in DMSO,6 months-80C in DMSO
Note: Products for research use only, not for human use
In Vitro TAS6417 inhibits the in vitro phosphorylation activity of EGFR and its mutants including an exon 20 insertion mutation, with IC50 values ranging from 1.10.1 to 8.01.1 nM. TAS6417 suppresses the growth of cells expressing exon 20 insertion mutations of the EGFR gene, with a GI50 value of 86.528.5 nM for LXF 2478L cells and 45.42.6 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 1.920.21 nM to 7.120.60 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. In Vivo 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.
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