Canertinib (CI-1033)
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.
Canertinib(也称CI-1033)是一种3-氯代、4-氟代的4-苯胺喹唑啉,是一种口服可用的、有效的和不可逆的Pan-erbB酪氨酸激酶抑制剂,可在体外抑制EGFR、HER2和HER4,半数最大抑制浓度IC50分别为0.8 nM、19 nM和7 nM[1]。
Canertinib不可逆地结合erbB 家族TK结构域的ATP口袋,canertinib的C6位点的丙烯酰胺侧链与erbB家族的半胱氨酸靠近,迅速形成共价键,使erB1、erB2和erB4家族成员永久失去催化活性,有效抑制erbB3依赖的信号通路[2]。
参考文献:
[1] Michelle Arkin, Mark M. Moasser. HER2 directed small molecule antagonists. Curr Opin Investig Drugs. Author manuscript; available in PMC 2011 February 1. Published in final edited form as: Curr Opin Investig Drugs. 2008 December; 9(12): 1264–1276.
[2] Calvo E, Tolcher AW, Hammond LA, Patnaik A, de Bono JS, Eiseman IA, Olson SC, Lenehan PF, McCreery H, Lorusso P, Rowinsky EK. Administration of CI-1033, an irreversible pan-erbB tyrosine kinase inhibitor, is feasible on a 7-day on, 7-day off schedule: a phase I pharmacokinetic and food effect study. Clin Cancer Res. 2004 Nov 1;10(21):7112-20.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 485.94 |
Cas No. | 267243-28-7 |
Formula | C24H25ClFN5O3 |
Solubility | insoluble in H2O; ≥10.1 mg/mL in EtOH; ≥12.15 mg/mL in DMSO with gentle warming |
Chemical Name | N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide |
SDF | Download SDF |
Canonical SMILES | C=CC(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4 |
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 | Canertinib是一种不可逆的喹唑啉基类HER家族酪氨酸激酶抑制剂,对EGFR、HER2和HER4的IC50值分别为0.8、19和7 nM。 | |||||
靶点 | EGFR | HER2 | HER4 | |||
IC50 | 0.8 nM | 19 nM | 7 nM |
质量控制和MSDS
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