RGNCY-0053 (Transtinib EGFR-TK inhibitor)

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Transtinib is a novel irreversible EGFR tyrosine kinase inhibitor.  Transtinib displays strong antiproliferative activity against the H1975 and A431 cell lines with IC50 of 34 nM and 62 nM respectively. Transtinib also significantly reduced tumor size for a prolonged period of time in xenograft models. Together, the results suggest that Trantinib is a potential cancer lead drug for the inhibition of EGFR to overcome the development of resistance.

Systematic Name: (S,E)-N-(4-((3-chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)-7-ethoxyquinolin-6-yl)-3-(pyrrolidin-2-yl)acrylamide

SMILES:  CCOC1=C(NC(/C=C/[C@H]2NCCC2)=O)C=C3C(N=CC=C3NC4=CC(Cl)=

C(OCC5=CC(F)=CC=C5)C=C4)=C1

Formula: C31H30ClFN4O3

Mol Wt: 561.05

PMID:   26848869