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Lazertinib

Catalog No.: 512194
Cas No.: 1903008-80-9
Purity : 98% Min.
512194 - Lazertinib | CAS 1903008-80-9

Catalog number : 512194

CAS number : 1903008-80-9

Molecular Formula : C30H34N8O3

Molecular Weight : 554.64

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

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

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SynonymsLazertinib; YH-25448; YH 25448; YH25448; GNS-1480; GNS 1480; GNS1480.
Molecular Formula C30H34N8O3
Molecular Weight554.64
Appearancelight-yellow to off-white solid 
Purity98% Min.
SolubilitySoluble in DMSO
StorageDry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shipping ConditionShipped under ambient temperature
SmileC=CC(NC1=CC(NC2=NC=CC(N3N=C(C4=CC=CC=C4)C(CN(C)C)=C3)=N2)=C(OC)C=C1N5CCOCC5)=O
InChiKeyRRMJMHOQSALEJJ-UHFFFAOYSA-N
InChiInChI=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)
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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


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.


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