AG-879
货号：
IA3030
品牌：
Jinpan
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产品简介
| MDL | MFCD00236450 |
| 描述 | 是酪氨酸激酶的抑制剂，能够抑制TrKA的磷酸化，但不能抑制TrKB 和TrKC，也是高选择性的ErbB2激酶抑制剂。 |
| 别名 | AG 879 |
| CAS | 148741-30-4 |
| 分子式 | C18H24N2OS |
| 分子量 | 316.46 |
| 纯度 | BR≥98% |
| 单位 | 瓶 |
| 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 | 10 μM (TrKA phosphorylation)[1]；1 μM (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] |
| SMILES | S=C(N)/C(C#N)=C/C1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 |
| 靶点 | Trk Receptor; ErbB2 |
| 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].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 also induces a dose-dependent increase in apoptosis with the exception of the lines TE-671 and HTB-88 cells[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]. |
| 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. |
| 规格 | 5mg 10mg 25mg |
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。