Lazertinib mesylate hydrate

Overview

Lazertinib (YH25448; GNS-1480) mesylate hydrate 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 hydrate 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 hydrate induces cell cycle arrest, apoptosis , spontaneous calcium responses, hyperexcitability of dorsal root ganglion ( DRG ) neurons, and TRPA1 -dependent pain-like behaviors. Lazertinib mesylate hydrate 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 hydrate 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 > Apoptosis | Products > Signaling Pathways > PI3K/Akt/mTOR | Products > Signaling Pathways > Neuronal Signaling | Products > Signaling Pathways > Membrane Transporter/Ion Channel | Products > Signaling Pathways > Protein Tyrosine Kinase/RTK | Products > Signaling Pathways > JAK/STAT Signaling | Products > Signaling Pathways > MAPK/ERK Pathway | Products > Signaling Pathways > Stem Cell/Wnt | Products > Research Areas > Cancer | Products > Signaling Pathways > Apoptosis | Products > Signaling Pathways > Akt | Products > Signaling Pathways > TRP Channel | Products > Signaling Pathways > EGFR | Products > Signaling Pathways > ERK

Product Information

• Catalog No.: HY-109061A
• CAS No.: 2411549-88-5
• Molecular Formula: C31H40N8O7S
• Molecular Weight: 668.76
• Purity: 99.98%
• Storage: Please store the product under the recommended conditions in the Certificate of Analysis.

Source

Original product source