CAS:2222755-14-64-(5-(6-((6-Methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyrazin-2-yl)-6-((R)-morpholin-2-ylmethoxy)pyrazolo[1,5-a]pyridine-3-carbonitrile

Synonyms: ARRY-192; RET-IN-1

LOXO-292 is a RET kinase inhibitor with IC50s of 1 nM, 7 nM, and 101 nM for RET (WT), RET (V804M) , and RET (G810R), respectively .

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18817579266

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18817579266

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描述RET fusions are validated therapeutic targets in human lung cancers. LOXO292 is a potent and highly selective RET inhibitor with IC50 values of 1nM, 7nM and 101nM for RET(WT), RET(V804M) and RET(G810R), respectively. It exhibited anti-tumor activity in the brain and periphery in RET-dependent tumor models in vivo.
动物研究
剂量
Nude Mice: 3 mg/kg - 50 mg/kg^[1] (p.o., BID)

给药途径
p.o.