iRGD peptide 1 TFA is the prototypic tumor-specific tissue-penetrating peptide, which delivers drugs deep into extravascular tumor tissue. iRGD peptide 1 TFA has anti-metastatic activity[1].
体外研究 (In Vitro)
iRGD peptide 1 (iRGD) inhibits migration of tumor cells and caused chemorepulsion in vitro in a CendR- and NRP-1-dependent manner. iRGD peptide 1 induces dramatic collapse of cellular processes and partial cell detachment, resulting in the repellent activity. These effects are prominently displayed when the cells are seeded on fibronectin, suggesting a role of CendR in functional regulation of integrins[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
iRGD peptide 1 (amino acid sequence: CRGDKGPDC; 4 μmol/kg; intravenous injection; every other day; for 21 days) potently inhibits spontaneous metastasis in mice[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
1064.08
Formula
C37H60F3N13O16S2
Sequence
Cys-Arg-Gly-Asp-Lys-Gly-Pro-Asp-Cys
Sequence Shortening
CRGDKGPDC
运输条件
Room temperature in continental US; may vary elsewhere.
iRGD peptide is a 9-amino acid cyclic peptide, triggers tissue penetration of drugs by first binding to av integrins, then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties.
IC50 & Target
Integrin[1]
体外研究 (In Vitro)
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].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
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].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
[2]. Zhang L, et al. Combination of NRP1-mediated iRGD with 5-fluorouracil suppresses proliferation, migration and invasion of gastric cancer cells. Biomed Pharmacother. 2017 Sep;93:1136-1143.
Animal Administration [2]
Mice[2] 12 male BALB/c nude mice (4-week-old) are assigned to 4 groups with 3 mice in each group. Among them,two groups are subcutaneously injected into the flanks by 3 × 106 HCG27 cells, the other two groups are conducted by NCI-N87 cells. Experimental groups are intravenously injected by 5-FU (25 mg/kg) mixed with iRGD peptide (4 mmol/kg) at every three days for 4 weeks while control groups are treated by 5-FU (25 mg/kg) mixed with PBS. And tumor volume is computed every 1 week with a digital vernier caliper using the following formula: tumor volume = (length × width2)/2[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
[2]. Zhang L, et al. Combination of NRP1-mediated iRGD with 5-fluorouracil suppresses proliferation, migration and invasion of gastric cancer cells. Biomed Pharmacother. 2017 Sep;93:1136-1143.
