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RG-14620

 
Catalog No.
C4766
表皮生长因子(EGF)受体激酶抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 600.00
Ship with 10-15 days
10mg
¥ 872.00
Ship with 10-15 days
50mg
¥ 3,272.00
Ship with 10-15 days

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A

背景

RG-14620 is a tyrosine kinase and epidermal growth factor (EGF) receptor [1].

Protein tyrosine kinases (PTKs) have been involved in regulating cell proliferation, cell differentiation, and signaling processes in the immune system. Dysfunction of protein tyrosine kinases result in inflammatory responses and diseases including cancer, atherosclerosis, and psoriasis [2]. The epidermal growth factor receptor (EGFR) is a transmembrane glycoprotein. Activation of EGFR results in autophosphorylation of receptor tyrosine kinase and has been involved in regulating cellular proliferation, differentiation, and survival. Overexpression of EGFR has been identified in a variety of tumor cell lines and has been associated with poor prognosis and decreased survival [3].

RG-14620 inhibited the activity of epidermal growth factor (EGF) receptor kinase with an IC50 value of 3 μM in HT-22 cells [1]. RG-14620 suppressed not only EGF-stimulated cancer cell proliferation in vitro but also tumor growth in nude mice [4]. Tyrphostin RG-14620 dose-dependently inhibited the EGFR-associated tyrosine kinase with half maximal inhibition at 7 μM [5].

References:
[1] Sagara, Y. , Ishige, K., Tsai, C., et al. Tyrphostins protect neuronal cells from oxidative stress. The Journal of Biological Chemisty, 277(39), 36204-36215(2002).
[2] Levitzki A, Gazit A.  Tyrosine kinase inhibition: an approach to drug development[J]. Science, 1995, 267(5205): 1782.
[3] Herbst R S.  Review of epidermal growth factor receptor biology[J]. International Journal of Radiation Oncology Biology Physics, 2004, 59(2): S21-S26.
[4] Yoneda T, Lyall R M, Alsina M M, et al.  The antiproliferative effects of tyrosine kinase inhibitors tyrphostins on a human squamous cell carcinoma in vitro and in nude mice[J]. Cancer research, 1991, 51(16): 4430-4435.
[5] Piontek M, Hengels K J, Porschen R, et al.  Antiproliferative effect of tyrosine kinase inhibitors in epidermal growth factor-stimulated growth of human gastric cancer cells[J]. Anticancer research, 1992, 13(6A): 2119-2123.

化学属性

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt275.1
Cas No.136831-49-7
FormulaC14H8Cl2N2
Solubility≤1mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide
Chemical Nameα-[(3,5-dichlorophenyl)methylene]-3-pyridineacetonitrile
SDFDownload SDF
Canonical SMILESClC1=CC(/C=C(C#N)/C2=CN=CC=C2)=CC(Cl)=C1
运输条件 蓝冰运输或根据您的需求运输。
一般建议不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

质量控制

质量控制和MSDS

批次:

化学结构

RG-14620