WZ-3146

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Chemical Structure| 1214265-56-1 同义名 : -
CAS号 : 1214265-56-1
货号 : A635130
分子式 : C24H25ClN6O2
纯度 : 99%+
分子量 : 464.947
MDL号 : MFCD18074503
存储条件：

Pure form Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(129.05 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • EGFR/ErbB1

    EGFR (E746_A750), IC50:2 nM

    EGFR (E746_A750/T790M), IC50:14 nM
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 p145met 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.22mL

10.75mL

2.15mL

1.08mL

21.51mL

4.30mL

2.15mL
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.