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AST-1306 TsOH
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 TsOH图片
CAS NO:1050500-29-2
包装与价格：
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
AST-1306 TsOH (AST-1306 (TsOH)) 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 TsOH 还抑制 ErbB4，IC50 为 0.8 nM。 AST-1306 TsOH 是一种苯胺基-喹唑啉化合物，具有抗癌活性
Cas No.1050500-29-2
别名艾力替尼; AST-1306 (TsOH)
化学名N-[4-[3-chloro-4-[(3-fluorophenyl)methoxy]anilino]quinazolin-6-yl]prop-2-enamide;4-methylbenzenesulfonic acid
Canonical SMILESCC1=CC=C(C=C1)S(=O)(=O)O.C=CC(=O)NC1=CC2=C(C=C1)N=CN=C2NC3=CC(=C(C=C3)OCC4=CC(=CC=C4)F)Cl
分子式C31H26ClFN4O5S
分子量621.08
溶解度DMF: 25 mg/ml,DMF:PBS (pH 7.2) (1:3): 0.25 mg/ml,DMSO: 20 mg/ml,Ethanol: 1 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

AST-1306 is a selective, irreversible inhibitor of ErbB2 and EGFR with IC50 values of 0.5nM and 3nM, respectively [1].

AST-1306 is designed and synthesized based on the chemical structure of lapatinib. The molecular docking method shows AST-1306 binds to the ATP-binding pocket of the kinases and form covalent bind with certain amino acids. AST-1306 can inhibit EGFR and ErbB2 in a cell-free assay with more than 3000-fold selectivity to other kinases. Besides the wild-type EGFR, AST-1306 also inhibits EGFR mutant T790M/L858R both in a cell-free assay and in HIH3T3 cells. The growth of the cells is suppressed by AST-1306 due to the inhibition of the phosphorylation of EGFR. It also occurs in some human cancer cells. Experiments have proved that AST-1306 notly inhibits the phosphorylation of EGFR and ErbB2 and subsequently decreases the downstream pathways of these kinases in A549 cells, Calu-3 cells and SK-OV-3 cells. Moreover, AST-1306 potently inhibits the tumor growth both in ErbB2-overexpressing xenograft models and FVB-2/Nneu transgenic mouse model [1].

References:
[1] Xie H, Lin L, Tong L, Jiang Y, Zheng M, Chen Z, Jiang X, Zhang X, Ren X, Qu W, Yang Y, Wan H, Chen Y, Zuo J, Jiang H, Geng M, Ding J. 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.