AST-1306 TsOH
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AST-1306是一种选择性的ErbB2和EGFR的不可逆抑制剂，IC50值分别为0.5 nM和3 nM[1]。
AST-1306是基于lapatinib的化学结构被设计和合成出来的。分子对接法显示AST-1306可结合激酶的ATP结合口袋，与某些氨基酸形成共价键。AST-1306可在无细胞的实验中抑制EGFR和ErbB2，比对其他激酶的亲和性高3000多倍。除野生型EGFR外，AST-1306也可在无细胞实验和HIH3T3细胞中结合EGFR突变体T790M/L858R。通过抑制EGFR的磷酸化，AST-1306可抑制细胞的生长。该现象在一些人类癌细胞中也出现。实验证明AST-1306可在A549细胞、Calu-3细胞和SK-OV-3细胞中显著地抑制EGFR和ErbB2磷酸化，进而减弱这些激酶的下游通路。此外，AST-1306可在ErbB2过表达的异种移植模型和FVB-2/Nneu转基因小鼠模型中有效抑制肿瘤生长[1]。
参考文献：
[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.
| Storage | Store at -20°C |
| M.Wt | 621.08 |
| Cas No. | 1050500-29-2 |
| Formula | C31H26ClFN4O5S |
| Solubility | Soluble in DMSO |
| Chemical Name | N-[4-[3-chloro-4-[(3-fluorophenyl)methoxy]anilino]quinazolin-6-yl]prop-2-enamide;4-methylbenzenesulfonic acid |
| SDF | Download SDF |
| Canonical SMILES | CC1=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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | AST-1306 TsOH是一种选择性的ErbB2和EGFR的不可逆抑制剂，IC50值分别为0.5 nM和3 nM。 | |||||
| 靶点 | ErbB2 | EGFR | ||||
| IC50 | 0.5 nM | 3 nM | ||||
化学结构
