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Lazertinib

编号: 512194
Cas号: 1903008-80-9
纯度: 98% Min.

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

仅供研究使用。 我们不向患者出售。

化学信息

名称Lazertinib
Iupac 化学名称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
同义词Lazertinib; YH-25448; YH 25448; YH25448; GNS-1480; GNS 1480; GNS1480.
英文同义词Lazertinib; YH-25448; YH 25448; YH25448; GNS-1480; GNS 1480; GNS1480.
分子式 C30H34N8O3
分子量554.64
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)
Cas号1903008-80-9
相关CAS号

订购信息

包装价格库存纯度备货期
大货询价询价询价
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外观性状浅黄色固体
纯度98% Min.
存储短期可在0-4度保存,数天至数月;长期可在-20度保存三年。
可溶性可溶于DMSO
处理方式
运输条件可在常温下运输
海关编码
Coming soon.
Targets
Mechanism
Cell study
Animal study
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.


化学结构

512194 - Lazertinib | CAS 1903008-80-9

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