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CAS No.: 148741-30-4

Tyrphostin AG 879 Catalog No. CSN12170

Synonyms: AG 879

Tyrphostin AG 879 potently inhibits HER2/ErbB2 with IC50 of 1 μM, 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 HER2

IC50:1μM
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].

动物研究

剂量

Mice: 5 mg/kg^[5] (i.p.), 100 mg/kg^[6] (s.c.); rat^[7] (s.c.): 6.7 mg/kg

给药途径

i.p., s.c.

动物药代数据

Animal	Mice^[6]
Dose	1 mg or 2 mg in liposomes
Administration	s.c.
T_1/2	2.6 h
T_max	4 h

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.1599 mL
- 15.7997 mL
- 31.5995 mL
- 5 mM
- 0.6320 mL
- 3.1599 mL
- 6.3199 mL
- 10 mM
- 0.3160 mL
- 1.5800 mL
- 3.1599 mL

技术信息

CAS号

148741-30-4

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H24N2OS

运输

蓝冰

分子量

316.46

别名

AG 879

溶解度

DMSO	36.0 mg/mL (113.8 mM)
Water	Insoluble
Ethanol	3.0 mg/mL (9.5 mM)

动物实验配方

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