Lazertinib
Description：Lazertinib is a an orally available third-generation, selective inhibitor of certain forms of the epidermal growth factor receptor (EGFR) with activating mutations, including the resistance mutation T790M, exon 19 deletions (Del19), and the L858R mutation, with potential antineoplastic activity. Upon administration, lazertinib specifically and irreversibly binds to and inhibits selective EGFR mutants, which prevents EGFR mutant-mediated signaling and leads to cell death in EGFR mutant-expressing tumor cells. Lazertinib may inhibit programmed cell death-1 ligand 1 (PD-L1) and inflammatory cytokines in specific cancer cells harboring certain EGFR mutations. Compared to some other EGFR inhibitors, lazertinib may have therapeutic benefits in tumors with T790M- or L858R-mediated drug resistance. In addition, lazertinib penetrates the blood-brain barrier (BBB). This agent shows minimal activity against wild-type EGFR (wtEGFR), and does not cause dose-limiting toxicities, which occur during the use of non-selective EGFR inhibitors and inhibit wtEGFR. EGFR, a receptor tyrosine kinase (RTK) mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.
Clinical Trial：Phase 1|Phase 2
Target：EGFR
For research use only. We do not sell to patients.
Chemical Information
| Name | Lazertinib |
|---|---|
| Iupac Chemical Name | N-{5-[(4-{4-[(dimethylamino)methyl]-3-phenyl-1H-pyrazol-1-yl}pyrimidin-2-yl)amino]-4-methoxy-2-(morpholin-4-yl)phenyl}prop-2-enamide |
| Synonyms | Lazertinib; YH-25448; YH 25448; YH25448; GNS-1480; GNS 1480; GNS1480. |
| Molecular Formula | C30H34N8O3 |
| Molecular Weight | 554.64 |
| Smile | C=CC(NC1=CC(NC2=NC=CC(N3N=C(C4=CC=CC=C4)C(CN(C)C)=C3)=N2)=C(OC)C=C1N5CCOCC5)=O |
| InChiKey | RRMJMHOQSALEJJ-UHFFFAOYSA-N |
| InChi | InChI=1S/C30H34N8O3/c1-5-28(39)32-23-17-24(26(40-4)18-25(23)37-13-15-41-16-14-37)33-30-31-12-11-27(34-30)38-20-22(19-36(2)3)29(35-38)21-9-7-6-8-10-21/h5-12,17-18,20H,1,13-16,19H2,2-4H3,(H,32,39)(H,31,33,34) |
| CAS Number | 1903008-80-9 |
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Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | light-yellow to off-white solid |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature |
| HS Code |
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| Mechanism | |
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| Clinical study |
1. N Engl J Med 372;18 nejm.org April 30, 2015; AZD9291 in EGFR Inhibitor–Resistant Non–Small-Cell Lung Cancer.
2. AACR 2018 Annual Meeting Abstract Number 4790: YH25448, an irreversible 3rd-generation EGFR TKI, exhibits superior anticancer effects with potent brain BBB penetration in NSCLC.
About Lazertinib
Lazertinib (YH25448, GNS-1480) is an oral, potent, highly mutant-selective and irreversible, investigational 3rd-generation EGFR-TKI that penetrates the blood-brain barrier (BBB). It targets the activating EGFR mutations Del19 and L858R, as well as the T790M mutation, while sparing wild type. EGFR mutations are present in approximately 10-15% of NSCLCs. Lazertinib is being evaluated in advanced NSCLC as both first- and second-line treatments.
Chemical Structure
