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AST-1306
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AST-1306图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议

产品介绍
AST-1306 (AST-1306) 是一种具有口服活性且不可逆的 EGFR 和 ErbB2 抑制剂,IC50 分别为 0.5 和 3 nM。 AST-1306 还抑制 ErbB4,IC50 为 0.8 nM。 AST-1306 是一种苯胺基-喹唑啉化合物,具有抗癌活性。

Cell experiment:

Cells are seeded into 96-well plates and grown for 24 h. The cells are then treated with increasing concentrations of Allitinib (AST1306) and grown for a further 72 h. Cell proliferation is evaluated using the SRB (Sulforhodamine B) assay[1].

Animal experiment:

Mice: Mice are administered Allitinib (AST1306) at dosage of 100, 50 and 25 mg/kg twice daily and treated with lapatinib (50 mg/kg) as comparison. Tumors are measured twice a week in two dimensions, using a caliper, and the tumor volume is calculated according to the formula L×W×W/2[1].

产品描述

AST1306 is a novel inhibitor of EGFR and HER2 (IC50 = 0.5 nM and 3 nM respectively)

EGFR (epidermal growth factor receptor) is a cell-surface receptor tyrosine kinase. The receptor activation leads to dimerization and tyrosine autophosphorylation. It induces a cascade of downstream cellular responses such as modification in gene expression, cell proliferation and cytoskeletal rearrangement etc. HER2 is a member of the epidermal growth factor and is associated with breast and ovarian cancers.

AST1306 selectively blocked EGFR and HER2 kinase activities in a cell-free assay. The tyrosine kinase activity of EGFR mutant T790M/L858R was also inhibited by AST1306 in intact cell and cell-free assays. In addition, AST1306 attenuated the EGFR and HER2 phosphorylation and downstream substrates. [1]

In ErbB2-overexpressing xenograft and FVB-2/Nneu transgenic mouse model, AST1306 potently inhibited tumor growth. In SK-OV-3 xenograft model, AST1306 caused a quick and long-lasting (≥24h) inhibition of EGFR and HER2. [1]

Reference:
1. Xie H, Lin L, Tong L et al.  AST1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo. PLoS One. 2011;6(7):e21487.