Lazertinib mesylate

Overview

Lazertinib (YH25448; GNS-1480) mesylate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate exhibits IC 50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2 , respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET , Lazertinib mesylate induces cell cycle arrest, apoptosis , spontaneous calcium responses, hyperexcitability of dorsal root ganglion ( DRG ) neurons, and TRPA1 -dependent pain-like behaviors. Lazertinib mesylate competitively binds to the substrate-binding sites of ABCB1/ABCG2 , stimulates their ATP ase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1 -mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate is applicable to research related to non-small cell lung cancer , multidrug-resistant cancers, and paresthesia.

Application

Products | Products > Disease Areas > Cancer | Products > Disease Areas > Respiratory Disease | Products > Disease Areas > Lung Cancer | Products > Disease Areas > Respiratory Cancer | Products > Disease Areas > Non-Small Cell Lung Cancer | Products > Signaling Pathways > Membrane Transporter/Ion Channel | Products > Signaling Pathways > Neuronal Signaling | Products > Signaling Pathways > Protein Tyrosine Kinase/RTK | Products > Signaling Pathways > JAK/STAT Signaling | Products > Signaling Pathways > PI3K/Akt/mTOR | Products > Signaling Pathways > Stem Cell/Wnt | Products > Signaling Pathways > MAPK/ERK Pathway | Products > Signaling Pathways > Apoptosis | Products > Research Areas > Cancer | Products > Signaling Pathways > TRP Channel | Products > Signaling Pathways > EGFR | Products > Signaling Pathways > Akt | Products > Signaling Pathways > ERK | Products > Signaling Pathways > Apoptosis

Product Information

• Catalog No.: HY-109061B
• CAS No.: 2247995-37-3
• Molecular Formula: C31H38N8O6S
• Molecular Weight: 650.75
• Purity: 99.85%
• Storage: 4°C, sealed storage, away from moisture * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
• Availability: In-stock

Source

Original product source