AG-879

AG-879

货号:
IA3030

品牌:
Jinpan

AG-879

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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
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。