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Tyrphostin AG 879

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Chemical Structure| 148741-30-4 同义名 : AG 879
CAS号 : 148741-30-4
货号 : A153685
分子式 : C18H24N2OS
纯度 : 95%
分子量 : 316.461
MDL号 : MFCD00236450
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(158 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • HER2

    HER2-Neu, IC50:1.0 μM
描述 Human epidermal growth factor receptor (EGFR; HER1,erbB1), human epidermal growth factor r eceptor 2 (HER2; erbB2), HER3 (erbB3) and HER4 (erbB4) are members of the ErbB family of transmembrane receptor tyrosine kinases. Among them, HER2 is a validated and high-value target. Approximately 30% of breast cancers have an amplification of the HER2/neu gene or overexpression of its protein product, HER2. Also, overexpression of HER2 occurs in gastric, colorectal, NSCLC and ovarian cancers. Tyrphostin AG 879 is a dual HER2 and Trk inhibitor with IC50 values of 1μM and 10μM, respectively[1]. Treatment with 100μM Tyrphostin AG879 in PC12 cells showed inhibition of Trk-A phosphorylation[2]. Exposure to 20μM Tyrphostin AG 879 for 24h led to decreased phosphorylation of ERK-1 and 2 and decreased protein levels of RAF-1 and HER-2 in MCF-7 cells. Tyrphostin AG 879 at concentration<20μM dose-dependently reduced cell growth of MCF-7, MDA-MB-231 and SK-BR-3 cells[3]. Blocking Trk in vivo by ICV infusions of Tyrphostin AG879 (10μl, 0.5mM in DMSO 10% (V/V) in PBS) impaired both short-term and long-term recognition memory[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.16mL

0.63mL

0.32mL

15.80mL

3.16mL

1.58mL

31.60mL

6.32mL

3.16mL
参考文献

[1]Levitzki A, Gazit A, et al. Tyrosine kinase inhibition: an approach to drug development. Science. 1995 Mar 24;267(5205):1782-8.

[2]Ohmichi M, Pang L, et al. The tyrosine kinase inhibitor tyrphostin blocks the cellular actions of nerve growth factor. Biochemistry. 1993 May 4;32(17):4650-8.

[3]Larsson LI, et al. Novel actions of tyrphostin AG 879: inhibition of RAF-1 and HER-2 expression combined with strong antitumoral effects on breast cancer cells. Cell Mol Life Sci. 2004 Oct;61(19-20):2624-31.

[4]Callaghan CK, Kelly AM, et al. Neurotrophins play differential roles in short and long-term recognition memory. Neurobiol Learn Mem. 2013 Sep;104:39-48.

[5]Kumar N, Sharma NR, et al. Receptor tyrosine kinase inhibitors that block replication of influenza a and other viruses. Antimicrob Agents Chemother. 2011 Dec;55(12):5553-9.

[6]Rende M, Pistilli A, 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.

[7]Neurotrophin NT3 promotes ovarian primordial to primary follicle transition