An inhibitor of mutant EGFRs; selective for EGFR mutant cell lines

Nazartinib – 5 mg

Brand:
Cayman
CAS:
1508250-71-2
Storage:
-20
UN-No:
Non-Hazardous - /

Nazartinib is an irreversible inhibitor of mutant EGF receptors (EGFRs).{43039} It is selective for EGFR mutant cell lines, including H3255 and HCC827 lung adenocarcinoma cells (IC50s = 6.11 and 1.52 nM, respectively) and resistant H1975 non-small cell lung cancer cells (NSCLC; IC50 = 4.18 nM), over cells expressing wild-type EGFRs (IC50 = 160.6 nM for HaCaT keratinocytes). Nazartinib decreases phosphorylation of EGFR in H3255, HCC827, and H1975 cells (EC50s = 5, 1, and 3 nM, respectively) and inhibits cell proliferation (EC50s = 9, 11, and 25 nM, respectively) but does not affect cell proliferation in cell lines containing wild-type EGFR.{43040} It reduces tumor growth in an HCC827 lung adenocarcinoma mouse xenograft model when administered at doses ranging from 3 to 100 mg/kg per day for 21 days.  

 

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Description

An inhibitor of mutant EGFRs; selective for EGFR mutant cell lines, including H3255 and HCC827 lung adenocarcinoma cells (IC50s = 6.11 and 1.52 nM, respectively) and resistant H1975 NSCLC cells (IC50 = 4.18 nM), over cells expressing wild-type EGFR (IC50 = 160.6 nM for HaCaT keratinocytes); decreases phosphorylation of EGFR in H3255, HCC827, and H1975 cells (EC50s = 5, 1, and 3 nM) and inhibits cell proliferation of H3255, HCC827, and H1975 cells (EC50s = 9, 11, and 25 nM) but does not affect cell proliferation in cell lines containing wild-type EGFR; reduces tumor growth in an HCC827 lung adenocarcinoma mouse xenograft model at doses ranging from 3 to 100 mg/kg per day

Formal name: N-[7-chloro-1-[(3R)-1-[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]hexahydro-1H-azepin-3-yl]-1H-benzimidazol-2-yl]-2-methyl-4-pyridinecarboxamide

Synonyms: 

Molecular weight: 495

CAS: 1508250-71-2

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||Research Area|Cancer|Multidrug Resistance

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