肿liu靶向肽 iRGD peptide环肽 1392278-76-0 c(CRGDKGPDC)

【中文名称】

RGD环肽

【英文名称】

c(CRGDKGPDC)，iRGD peptide

【CAS】

1392278-76-0

【单字母】

H2N-CRGDKGPDC-OH(Disulfide Bridge:C1-C9)

【三字母】

 H2N-Cys-Arg-Gly-Asp-Lys-Gly-Pro-Asp-Cys-COOH(Disulfide Bridge:Cys1-Cys9)

【氨基酸个数】

 9

【分子式】

C35H57N13O14S2

【平均分子量】

 948.04

【 分子量】

947.36

【等电点(PI)】

 8.83

【pH=7.0时的净电荷数】 

1.91

【平均亲水性】

 1.6666666666667

【疏水性值】

  -1.42

【外观与性状】

粉末状固体

【体内研究】

iRGD inserted in the oncolytic adenovirus ICOVIR15K (ICOVIR15K-iRGD) enhances early adenovirus dissemination through the tumor mass and elevates the antitumor effect in mice[1]. iRGD (4 mmol/kg, i.v.) in combination with 5-FU significantly suppresses the tumor growth in nude mice bearing human gastric cancer cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

【体外研究】

iRGD peptide-mediated tumor penetration occurs in three steps: binding to αv-integrins on tumor vasculature or tumor cells, exposure by proteolysis of a C-terminal motif that binds to neuropilin-1 (NRP-1) and cell internalization. iRGD peptide inserted in the ICOVIR15K fiber C terminus enhances binding and internalization only in MCF7 cells, which express NRP-1 and integrins. iRGD insertion does not impair virus infection and replication[1]. iRGD peptide alone has no obvious effect on gastric cancer cells, and when combined with 5-FU, iRGD peptide (0.3 μmol/mL) enhances the chemotherapy efficacy of 5-FU on gastric cancer cells through NRP1[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

【产品简介】

iRGD (CRGDKGPDC) (Disulfide bridge: C1-C9)是一种由 9 个氨基酸组成的二硫键环肽，由 位半胱氨酸C与末尾的C巯基之间氧化形成二硫键。它能够与整合素结合后酶解产生 CRGDK ，再与 神经纤毛蛋白-1 (neuropilin-1) 相互作用，从而促进药物的组织渗透，具有靶向肿liu以及肿liu渗透的作用。
iRGD和DSPE-PEG偶联后，DSPE-PEG-iRGD可以用来制作胶束，囊泡等纳米颗粒；iRGD-PEG-DSPE形成的脂质体可以直接作用于肿liu靶点，形成主动靶向效果。