BIBU 1361 dihydrochloride
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.
BIBU 1361盐酸盐是表皮生长因子受体(EGFR)激酶的选择性抑制剂,IC50值为0.038 ± 0.007 μM[1,2]。
表皮生长因子受体信号传导通路参与多种细胞内信号传导事件,促进增殖和存活,它在胶质母细胞瘤(GBM)的进展中发挥关键作用[2]。
在神经胶质瘤细胞,表皮生长因子受体信号可诱导Akt、ERK1/2和STAT3的磷酸化。BIBU 1361降低EGFR的水平,随后降低pP-EGFR的水平。这种效应伴随着pAkt和下游靶标p-mTOR的减少。P-S6激酶和p-P70S6激酶是p-mTOR的两个关键靶标,两者都与细胞增殖相关。只用BIBU 1361处理胶质瘤细胞,P-S6激酶和P-P70S6激酶下调。E2F1是G1/S调节剂。E2F1可与表皮生长因子受体相互作用。Akt/mTOR信号的抑制可影响细胞周期进程。在神经胶质瘤细胞中,BIBU 1361抑制AKT/mTOR的表达,降低表皮生长因子受体。在神经胶质瘤细胞中,BIBU 1361降低细胞周期蛋白E和E2F1的表达,增加p21的水平,并增加S期和G2/M期的细胞数[2]。
目前还没有发现动物体内BIBU 1361的作用。
参考文献:
[1]. Antczak C, Mahida JP, Bhinder B, et al. A High-Content Biosensor-Based Screen Identifies Cell-Permeable Activators and Inhibitors of EGFR Function Implications in Drug Discovery. Journal of biomolecular screening, 2012, 17(7): 885-899.
[2]. Ghildiyal R, Dixit D, Sen E. EGFR inhibitor BIBU induces apoptosis and defective autophagy in glioma cells. Molecular carcinogenesis, 2013, 52(12): 970-982.
Physical Appearance | Yellow solid |
Storage | Store at 4°C |
M.Wt | 516.87 |
Cas No. | 793726-84-8 |
Formula | C22H27ClFN7·2HCl |
Solubility | <51.69mg/ml in H2O; <12.92mg/ml in DMSO |
Chemical Name | N-(3-chloro-4-fluorophenyl)-6-(4-((diethylamino)methyl)piperidin-1-yl)pyrimido[5,4-d]pyrimidin-4-amine dihydrochloride |
SDF | Download SDF |
Canonical SMILES | ClC1=CC(NC2=NC=NC3=CN=C(N=C32)N4CCC(CN(CC)CC)CC4)=CC=C1F.Cl.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。 |