2411549-88-5
Chemical Structure
Lazertinib mesylate hydrate
Synonym(s): YH25448 mesylate hydrate; GNS-1480 mesylate hydrate
- CAS No.: 2411549-88-5
- Formula:C31H40N8O7S
- Molecular Weight:668.76
IUPAC Name: N-(5-((4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yl)pyrimidin-2-yl)amino)-4-methoxy-2-morpholinophenyl)acrylamide methanesulfonate hydrate
InChIKey: ZJPNGZUERUYZEG-UHFFFAOYSA-N
SMILES: O=C(NC1=CC(NC2=NC=CC(N3N=C(C(CN(C)C)=C3)C4=CC=CC=C4)=N2)=C(C=C1N5CCOCC5)OC)C=C.O=S(O)(C)=O.O
Biological Activity: 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 IC50 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 ATPase 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[1][2][3][4].
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Lazertinib mesylate hydrate | 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 IC50 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 ATPase 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. | |||||||||||||||||||||
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- [1]. Oh SY, et al. The potential of lazertinib and amivantamab combination therapy as a treatment strategy for uncommon EGFR-mutated NSCLC. Cell Rep Med. 2025;6(2):101929. [Content Brief]
- [2]. Matsui Y, et al. Initial AXL and MCL-1 inhibition contributes to abolishing lazertinib tolerance in EGFR-mutant lung cancer cells. Cancer Sci. 2024;115(10):3333-3345. [Content Brief]
- [3]. Fan Y, et al. Lazertinib improves the efficacy of chemotherapeutic drugs in ABCB1 or ABCG2 overexpression cancer cells in vitro, in vivo, and ex vivo[J]. Molecular Therapy-Oncolytics, 2022, 24: 636-649.
- [4]. Kim H, et al. EGFR Tyrosine Kinase Inhibitor Lazertinib Activates a Subset of Mouse Sensory Neurons Via TRPA1. J Pain. 2024;25(5):104435. [Content Brief]
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