| 生物活性： |
靶点：Trk Receptor; ErbB2
通路：Angiogenesis; Protein Tyrosine Kinase/RTK; JAK/STAT Signaling;Neuronal Signaling
背景说明：是酪氨酸激酶的抑制剂,能够抑制TrKA的磷酸化,也是高选择性的ErbB2激酶抑制剂。
生物活性：Tyrphostin AG 879 (AG 879) is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation (IC50 of 10 μM), but not TrKB and TrKC. Tyrphostin AG 879 is also a selective ErbB2 tyrosine kinase inhibitor with an IC50 of 1 μM, and has at least 500-fold higher selectivity to ErbB2 than EGFR. Tyrphostin AG 879 has anticancer activity[1-2].
IC50：10μM(TrKA phosphorylation)[1];1μM(ErbB2)[2]
In Vitro：在人平滑肌肉瘤(HTB-114，HTB-115，HTB-88)，横纹肌肉瘤(HTB-82，TE-671)，前列腺癌(PC-3)，急性早幼粒细胞白血病(HL-60)和组织细胞淋巴瘤(U-937)细胞系中，AG879(20 μM)显著减少细胞增殖，并使细胞凋亡不同程度地增加。[1] AG879浓度依赖性抑制FET6αS26X细胞的生长。[2]
In Vivo：在移植HTB-114 或 HL-60的无胸腺NOD/SCID小鼠体内，AG879(2 mg)减少肿瘤生长。[1]
细胞实验：Tyrphostin AG 879(100 mg/kg;subcutaneous injection; administered 10 times in 19 days; for 21 days; athymic，immunodepressed NOD/SCID female mice)treatment induces in vivo a decrease in cancer growth in grafted athymic NOD/SCID mice[1].
动物实验：Tyrphostin AG 879(0.5-50 μM; 48 hours; HL-60，U-937，PC-3，HTB-82，HTB-114，TE-671，HTB-115 and HTB-88 cells)treatment significantly and dose dependently decreases cell proliferation in all the cell lines[1].
数据来源文献：[1]. Rende M et al. Role of nerve growth factor and its receptors in non-nervous cancer growth: efficacy of a tyrosine kinase inhibitor (AG879) and neutralizing antibodies antityrosine kinase receptor A and antinerve growth factor: an in-vitro and in-vivo study. Anticancer Drugs. 2006 Sep;17(8):929-41.
[2]. Zhou Y et al. Blockade of EGFR and ErbB2 by the novel dual EGFR and ErbB2 tyrosine kinase inhibitor GW572016 sensitizes human colon carcinoma GEO cells to apoptosis. Cancer Res. 2006 Jan 1;66(1):404-11.
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