RGNCY-0035 (ALK Inhibitor)

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RGNCY-0035 is a potent inhibitor across a broad panel of engineered ALK mutant cell lines and showed suitable preclinical pharmacokinetics and robust tumor growth inhibition in a crizotinib-resistant cell line (H3122-L1196M).   A promising clinical candidate for treating crizotinib-sensitive and resistant ALK-positive NSCLC patients.

Systematic Name: 2-(5-(6-amino-5-((R)-1-(5-fluoro-2-(2H-1,2,3-triazol-2-yl)phenyl)ethoxy)pyridin-3-yl)-4-methylthiazol-2-yl)propane-1,2-diol

SMILES: NC1=NC=C(C2=C(C)N=C(C(O)(CO)C)S2)C=C1O[C@H](C)C3=C(N4N=CC=N4)C=CC(F)=C3

Formula: C22H23FN6O3S

Mol. Wt.: 470.52

PMID: 24498900

Reference: Lu, Xiaoyun, and Ke Ding. "Novel Anaplastic Lymphoma Kinase Inhibitors Targeting Clinically Acquired Resistance." Journal of Medicinal Chemistry 57.4 (2014): 1167-1169.

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