Chemical Name: 6-(2-Hydroxy-2-methylpropoxy)-4-[6-[6-[(6-methoxy-3-pyridinyl)methyl]-3,6-diazabicyclo[3.1.1]hept-3-yl]-3-pyridinyl]pyrazolo[1,5-a]pyridine-3-carbonitrile
Biological ActivitySelpercatinib, is a potent and selective receptor tyrosine kinase RET inhibitor (EC50 = 4 nM). It shows > 100-fold selectivity for > 95% of 228 purified kinase domains in radiometric assays. In vitro, it inhibits proliferation of cancer cell lines containing RET mutations or gene fusions. In vivo, it inhibits tumor growth in diverse RET mouse models. Selpercatinib is orally bioavailable.
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