WZ3146
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.
WZ3146是一种新型不可逆的抑制剂,可有效抑制EGFR(L858R)和EGFR(E746_A75)磷酸化,IC50值均为2 nM。
WZ3146可在非小细胞肺癌(NSCLC)细胞系中抑制EGFR磷酸化[1]。WZ3146可抑制包含EGFR T790M的细胞系生长。此外,对重组EGFR T790M激酶与WZ3146孵育的电喷雾质谱分析表明,一个抑制剂分子的化学计量数加入到蛋白中。修饰蛋白的胃蛋白酶消化串联质谱分析表明,Cys 797是修饰位点,表明WZ3146与EGFR之间形成共价键[2]。
参考文献:
[1] Thanyanan Reungwetwattana, Saravut J. Weroha, Julian R. Molina. Oncogenic Pathways, Molecularly Targeted Therapies, and Highlighted Clinical Trials in Non–Small-Cell Lung Cancer (NSCLC). Clinical Lung Cancer, Volume 13, Issue 4, July 2012, Pages 252-266
[2] Zhou W1, Ercan D, Chen L, Yun CH, Li D, Capelletti M, Cortot AB, Chirieac L, Iacob RE, Padera R, Engen JR, Wong KK, Eck MJ, Gray NS, Jnne PA. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009 Dec 24;462(7276):1070-4.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 464.95 |
Cas No. | 1214265-56-1 |
Formula | C24H25ClN6O2 |
Solubility | ≥23.25 mg/mL in DMSO with gentle warming |
Chemical Name | N-(3-((5-chloro-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)oxy)phenyl)acrylamide |
SDF | Download SDF |
Canonical SMILES | C=CC(NC1=CC=CC(OC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3)=NC=C2Cl)=C1)=O |
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 | WZ3146是一种有效的和不可逆的突变EGFR抑制剂,对EGFR(L858R)和EGFR(E746_A75)的IC50值均为2 nM。 | |||||
靶点 | EGFR(L858R) | EGFR(E746_A750) | ||||
IC50 | 2 nM | 2 nM |
质量控制和MSDS
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