AG 494

An inhibitor of EGF receptor kinase

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

库存: 现货

可选规格

包装

价格

促销价

数量
10mg

￥675.00

540.00

- +
50mg

￥3050.00

2440.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

货号: ajci19220
CAS: 133550-35-3
别名: Tyrphostin AG 494
分子式: C16H12N2O3
分子量: 280.28
纯度: >98%
溶解度: DMF: 30 mg/ml,DMF:PBS (pH7.2) (1:1): 0.5 mg/ml,DMSO: 20 mg/ml,Ethanol: 1 mg/ml
储存: 4°C, protect from light
库存: 现货

Background

AG 494 is a potent and selective inhibitor of EGFR with IC50 value of 0.7 μM.

The epidermal growth factor receptor (EGFR) is the cell-surface receptor for epidermal growth factor and plays an important role in tumor invasion and cancer cell proliferation.

AG 494 is a potent and selective EGFR inhibitor. AG 494 inhibited autophosphorylation of EGFR and HER-2 with IC50 values of 1.1 and 39 μM, respectively. In DHER-14 cells, AG 494 inhibited Cdk2 activation and EGF-dependent DNA synthesis [1]. AG494 arrested cells at late G1 and S phase and inhibited the activation of Cdk2 by phosphorylating tyrosine 15 on Cdk2 [2]. Epidermal growth factor (EGF) increased (bone morphogenetic protein) BMP9-induced osteogenic markers of mesenchymal stem cells (MSCs), which was inhibited by AG-494 in a time- and dose-dependent way [3]. In human prostate (DU145) and lung (A549) cancer cell lines, AG494 reversibly and significantly inhibited autocrine growth in a dose-dependent way. Also, AG494 induced cell apoptosis in both cell lines and arrested cell growth in the G1 phase [4].

参考文献:
[1].? Osherov N, Levitzki A. Tyrphostin AG 494 blocks Cdk2 activation. FEBS Lett, 1997, 410(2-3): 187-190.
[2].? Kleinberger-Doron N, Shelah N, Capone R, et al. Inhibition of Cdk2 activation by selected tyrphostins causes cell cycle arrest at late G1 and S phase. Exp Cell Res, 1998, 241(2): 340-351.
[3].? Liu X, Qin J, Luo Q, et al. Cross-talk between EGF and BMP9 signalling pathways regulates the osteogenic differentiation of mesenchymal stem cells. J Cell Mol Med, 2013, 17(9): 1160-1172.
[4].? Bojko A1, Reichert K, Adamczyk A, et al. The effect of tyrphostins AG494 and AG1478 on the autocrine growth regulation of A549 and DU145 cells. Folia Histochem Cytobiol, 2012, 50(2): 186-195.