2225887-26-1|EGFR-IN-5|CsnPharm

CAS No.: 2225887-26-1

EGFR-IN-5 Catalog No. CSN28785

Synonyms: EGFR-IN-5

EGFR-IN-5 is an inhibitor of EGFR with IC50 values of 10.4 nM, 1.1 nM, 34 nM and 7.2 nM for EGFR, EGFRL858R, EGFRL858R/T790M, and EGFRL858R/T790M/C797S, respectively. It could suppress EGFR phosphorylation in a dose-dependent manner in HCC827 cell line and significantly induce the apoptosis of HCC827 cells.

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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].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7492 mL
- 8.7460 mL
- 17.4920 mL
- 5 mM
- 0.3498 mL
- 1.7492 mL
- 3.4984 mL
- 10 mM
- 0.1749 mL
- 0.8746 mL
- 1.7492 mL

技术信息

CAS号	2225887-26-1	储存条件	粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C31H38FN9O	运输	蓝冰
分子量	571.69	别名	EGFR-IN-5

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