Lazertinib

Overview

Lazertinib (YH25448; GNS-1480) 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 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 induces cell cycle arrest, apoptosis , spontaneous calcium responses, hyperexcitability of dorsal root ganglion ( DRG ) neurons, and TRPA1 -dependent pain-like behaviors. Lazertinib 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 is applicable to research related to non-small cell lung cancer , multidrug-resistant cancers, and paresthesia.

Application

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Product Information

• Catalog No.: HY-109061
• CAS No.: 1903008-80-9
• Molecular Formula: C30H34N8O3
• Molecular Weight: 554.64
• Purity: 99.87%
• Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
• Solubility: ≥ 0.9 mg/mL (1.62 mM); Clear solution
• Availability: In-stock

Source

Original product source