An irreversible inhibitor of mutant EGFRs; inhibits cell proliferation of Ba/F3 cells expressing various EGFR mutations (IC50s= 9-11 nM); selective for mutant EGFRs over wild-type EGFR (IC50 = 830 nM); reduces phosphorylated levels of EGFR

Naquotinib – 1 mg

Brand:
Cayman
CAS:
1448232-80-1
Storage:
-20
UN-No:
De Minimis - 3077 / 9

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}  

 

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SKU: 23498 - 1 mg Category:

Description

An irreversible inhibitor of mutant EGFRs; inhibits cell proliferation of Ba/F3 cells expressing various EGFR mutations (IC50s= 9-11 nM); selective for mutant EGFRs over wild-type EGFR (IC50 = 830 nM); reduces phosphorylated levels of EGFR, AKT, and ERK and decreases cell viability in NSCLC cells and cells carrying an exon 20 insertion mutation; reduces tumor growth in PC-9/NaqRc2 mouse xenograft model at 50 mg/kg per day

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

Synonyms: 

Molecular weight: 562.7

CAS: 1448232-80-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|EGFR/ErbB/HER Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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