AG 494

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AG 494

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

133550-35-3

包装与价格：

包装	价格(元)
10mg	电议
50mg	电议

产品介绍

AG 494 (Tyrphostin AG 494) 是一种有效的选择性 EGFR 酪氨酸激酶抑制剂 (IC50\u003d0.7 μM)。 AG 494 抑制 EGFR、ErbB2、HER1-2 和 PDGF-R 的自磷酸化，IC5\u200b\u200b0 分别为 1.1、39、45 和 6 μM。 AG 494 阻断 Cdk2 活化并抑制 EGF 依赖性 DNA 合成。

Cas No.	133550-35-3
别名	Tyrphostin AG 494
化学名	(E)-2-cyano-3-(3,4-dihydroxyphenyl)-N-phenylacrylamide
Canonical SMILES	OC1=CC(/C=C(C#N)/C(NC2=CC=CC=C2)=O)=CC=C1O
分子式	C₁₆H₁₂N₂O₃
分子量	280.28
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
储存条件	4°C, protect from light
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	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]. References: [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.