Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: 6-ethyl-3-[[4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]amino]-5-[[(3R)-1-(1-oxo-2-propen-1-yl)-3-pyrrolidinyl]oxy]-2-pyrazinecarboxamide
Purity: ≥98%
Formula Markup: C30H42N8O3
Formula Weight: 562.7
CAS Number: 1448232-80-1
Notes: Naquotinib is an irreversible inhibitor of mutant EGF receptors (EGFRs).{36679} It inhibits proliferation of Ba/F3 cells expressing various EGFR mutations, including deletion of exon 19, deletion of exon 19 plus a T790M mutation, L858R, and L858R plus the T790M mutation (IC50s = 9, 10, 11, and 9 nM, respectively). It is selective for these mutations over the triple mutations that include exon 19 deletion plus T790M and C797S and L858R plus T790M and C797S and over wild-type EGFR (IC50s = 235, 1,994, and 830 nM, respectively). It reduces phosphorylated levels of EGFR, AKT, and ERK and decreases cell viability in non-small cell lung cancer (NSCLC) cells and in Ba/F3 cells carrying an exon 20 insertion mutation. Naquotinib (50 mg/kg per day) also reduces tumor growth in a PC-9/NaqRc2 mouse xenograft model.{36680}
Deutsch
English
