Name | iRGD |
Synonyms | iRGD iRGD TFA c(CRGDKGPDC) iRGD peptide TFA salt L-Cysteine, L-cysteinyl-L-arginylglycyl-L-α-aspartyl-L-lysylglycyl-L-prolyl-L-α-aspartyl-, cyclic (1→9)-disulfide |
CAS | 1392278-76-0 |
Molecular Formula | C35H57N13O14S2 |
Molar Mass | 948.04 |
Density | 1.68±0.1 g/cm3(Predicted) |
pKa | 2.92±0.70(Predicted) |
Storage Condition | Room Temprature |
In vitro study | 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. 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. |
In vivo study | iRGD inserted in the oncolytic adenovirus ICOVIR15K (ICOVIR15K-iRGD) enhances early adenovirus dissemination through the tumor mass and elevates the antitumor effect in mice. iRGD (4 mmol/kg, i.v.) in combination with 5-FU significantly suppresses the tumor growth in nude mice bearing human gastric cancer cells. |
biological activity | iRGD peptide is a cyclic peptide consisting of 9 amino acids, the subsequent enzymatic hydrolysis results in the interaction between CRGDK/R and neuropilin-1 (neuropilin-1), thereby promoting the tissue penetration of the drug, which has the effect of targeting tumor and tumor penetration. |
Target | Integrin |