|N-(3-((5-氯-2-((4-(4-甲基哌嗪-1-基)苯基)氨基)嘧啶-4-基)氧基)苯基)丙烯酰胺|CsnPharm

CAS No.: 1214265-56-1

WZ-3146 Catalog No. CSN16526

Synonyms: WZ3146

WZ3146 is a mutant-selective irreversible inhibitor of EGFR (L858R) and EGFR (E746_A750) with IC50 of 2 nM and 2 nM and does not inhibit ERBB2 phosphorylation (T798I).

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400-920-2911

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技术信息

生物活性

描述Epidermal Growth Factor Receptor (EGFR) is a transmembrane glycoprotein that constitutes one of the four members of ErbB family of tyrosine kinase receptors. Activation of EGFR leads to autophosphorylation of receptor tyrosine kinase that initiates a cascade of downstream signaling pathways involved in regulating cellular proliferation, differentiation, and survival. EGFR is abnormally activated by various mechanisms like receptor overexpression, mutation, ligand-dependent receptor dimerization, ligand-independent activation and is associated with the development of variety of human cancers^[2]. AG99 (α-cyano-(3,4-dihydroxy)cinnamide) is a potent EGFR inhibitor. It effectively blocks tyrosine phosphorylation of p145^met and promotes cell death accompanied by activation of caspase-like proteases^[4]. AG99 was shown to inhibit the appearance of pp145 (145-kDa protein) to some extent. It also showed a growth-inhibitory effect on not only serum-starved cells but also normally grown cells, which suggested, therefore, that the importance of EGFR is not limited to serum-independent growth and/or the EGFR inhibitor has an alternative target to exert its growth-inhibitory effect in normally grown cells^[4].
参考文献

[1] Zhou W, Ercan D, et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009 Dec 24;462(7276):1070-4.
[2] Singh D, Attri BK, Gill RK, Bariwal J. Review on EGFR Inhibitors: Critical Updates. Mini Rev Med Chem. 2016;16(14):1134-66. doi: 10.2174/1389557516666160321114917. PMID: 26996617.
[3] Park YH, Kim DK, Kim HS, et al. WZ3146 inhibits mast cell Lyn and Fyn to reduce IgE-mediated allergic responses in vitro and in vivo. Toxicol Appl Pharmacol. 2019;383:114763.
[4] Yamamoto N, Mammadova G, Song RX, Fukami Y, Sato K. Tyrosine phosphorylation of p145met mediated by EGFR and Src is required for serum-independent survival of human bladder carcinoma cells. J Cell Sci. 2006 Nov 15;119(Pt 22):4623-33. doi: 10.1242/jcs.03236. Epub 2006 Oct 24. PMID: 17062641.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1508 mL
- 10.7539 mL
- 21.5078 mL
- 5 mM
- 0.4302 mL
- 2.1508 mL
- 4.3016 mL
- 10 mM
- 0.2151 mL
- 1.0754 mL
- 2.1508 mL

技术信息

CAS号

1214265-56-1

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H25ClN6O2

运输

蓝冰

分子量

464.95

别名

WZ3146

溶解度

DMSO	210.0 mg/mL (451.7 mM)
Water	insoluble

动物实验配方

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