EGFR-IN-5

产品说明书

Print
Chemical Structure| 2225887-26-1 同义名 : -
CAS号 : 2225887-26-1
货号 : A1176711
分子式 : C31H38FN9O
纯度 : 99%+
分子量 : 571.692
MDL号 : MFCD31813637
存储条件：

Pure form Keep in dark place,Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 The epidermal growth factor receptor (EGFR), a member of the ErbB family (EGFR, ErbB2, ErbB3 and ErbB4), plays a crucial role in regulating various cellular responses such as proliferation, differentiation, and survival. As a result, aberrant activation of EGFR, mostly mediated through different classes of genomic alterations occurring within EGFR, is closely associated with the pathogenesis of numerous human cancers including lung adenocarcinoma, glioblastoma, and colorectal cancer[2]. The weight and relative volume of tumors in the epidermal growth factor receptor-tyrosine kinase inhibitor (EGFR-TKI) treated group were less than those in the solvent control group. The average lymphatic vessel density of EGFR-TKI-treated mice was 6.44 per case. This value was 10.70 per case in the solvent control group. Lower density of lymphangiogenesis was found in the EGFR-TKI treated group (P=0.023). The area and longest diameter of neonatal lymphatic vessel of the EGFR-TKI treated group were less than those of the solvent control group. Moreover, EGFR-TKI exhibited no significant effect on the invasion of tumor cells into the lymphatic vessel (P=0.519)[3]. Bile duct ligation (BDL) induced biliary infarcts and matrix deposition in mouse liver, and EGFR was expressed and phosphorylated by α-smooth muscle actin (αSMA)-positive myofibroblasts. LX-2 cells expressed EGFR, and these receptors were phosphorylated in the in vitro culture system. Growth curve and cell cycle analysis revealed that EGF could enhance cell proliferation of LX-2 cells[4]. EGFR-IN-5 is a EGFR inhibitor, with IC50s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFRL858R, EGFRL858R/T790M, and EGFRL858R/T790M/C797S, respectively[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.75mL

0.35mL

0.17mL

8.75mL

1.75mL

0.87mL

17.49mL

3.50mL

1.75mL
参考文献

[1]Zhang H, Wang J, Shen Y, Wang HY, Duan WM, Zhao HY, Hei YY, Xin M, Cao YX, Zhang SQ. Discovery of 2,4,6-trisubstitued pyrido[3,4-d]pyrimidine derivatives as new EGFR-TKIs. Eur J Med Chem. 2018 Mar 25;148:221-237. doi: 10.1016/j.ejmech.2018.02.051. Epub 2018 Feb 16. PMID: 29466773.

[2] Jeonghee Cho. Mechanistic insights into differential requirement of receptor dimerization for oncogenic activation of mutant EGFR and its clinical perspective. BMB Rep. 2020 Mar;53(3):133-141.

[3] Minghui Cai,et al. Effect of EGFR-TKI on lymphangiogenesis of lung cancer with EGFR mutation. Zhongguo Fei Ai Za Zhi. 2014 Dec;17(12):834-8.

[4] Hufeng Xu,et al. EGF neutralization antibodies attenuate liver fibrosis by inhibiting myofibroblast proliferation in bile duct ligation mice. Histochem Cell Biol. 2020 Jul;154(1):107-116.

[5]Zhang H, et al. Discovery of 2,4,6-trisubstitued pyrido[3,4-d]pyrimidine derivatives as new EGFR-TKIs. Eur J Med Chem. 2018 Mar 25;148:221-237.