EGFR Inhibitor

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EGFR Inhibitor

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。

CAS NO:

879127-07-8

包装与价格：

包装	价格(元)
1mg	电议
5mg	电议
25mg	电议

产品介绍

EGFR Inhibitor 是一种 4,6-二取代嘧啶，是一种有效的、ATP 竞争性的、不可逆的、高度选择性的 EGFR 抑制剂，IC50 为 21 nM。 EGFR Inhibitor 还抑制突变型 EGFRL858R 和 EGFRL861Q，IC50 分别为 63 nM 和 4 nM。 EGFR Inhibitor 对 EGFR 的选择性强于 HER4 (IC50 = 7640 nM) 和一组 55 种其他激酶。 EGFR Inhibitor 可诱导细胞凋亡并具有抗肿瘤活性。

Cas No.	879127-07-8
别名	Epidermal Growth Factor Receptor Inhibitor
化学名	N-[3-[[6-[[3-(trifluoromethyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-cyclopropanecarboxamide
Canonical SMILES	O=C(C1CC1)NC2=CC=CC(NC3=CC(NC4=CC(C(F)(F)F)=CC=C4)=NC=N3)=C2
分子式	C₂₁H₁₈F₃N₅O
分子量	413.4
溶解度	≤0.2mg/ml in ethanol;20mg/ml in DMSO;25mg/ml in dimethyl formamide
储存条件	Store at -20℃
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	EGFR inhibitor is a cell permeable, pyrimidine compound that selectively inhibits the EGFR kinase with IC50 value of 21 nM [1]. EGFR is a transmembrane protein, and is a receptor for members of epidermal growth factor family. The binding of EGFR with its ligands induces receptor dimerization and tyrosine autophosphorylation, and leads to cell proliferation. The overactivity of EGFR tyrosine kinases is associated with a number of cancers, inhibition of EGFR can downregulate antiapoptotic proteins such as surviving and upregulate proapoptotic proteins such as Bim. Thus, EGFR inhibitor can induce cell apoptosis, resulting in anti-tumor effectivity [2]. EGFR inhibitor inhibited EGFR kinase in vitro and blocks receptor autophosphorylation in cells. EGFR inhibitor also inhibited L858R and L861Q EGFR mutants with IC50 values of 63 and 4 nM, respectively [1]. References: 1. Q. Zhang, Y. Liu, F. Gao, et al. Discovery of EGFR selective 4,6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle library. Journal of the American Chemical Society 128(7), 2182-2183 (2006). 2. F. Ciardiello, G. Tortora. EGFR antagonists in cancer treatment. New England Journal of Medicine 358(11), 1160-1174 (2008).