iRGD peptide

iRGD peptide

• COA/MS/HPLC Report
• Handling and Storage of Synthetic Peptides
• Material Safety Data Sheets (MSDS)

Batch to batch variation of the purity

c(CRGDKGPDC) (Disulfide bridge:Cys1-Cys9)

H-Cys-Arg-Gly-Asp-Lys-Gly-Pro-Asp-Cys-OH (Disulfide bridge:Cys1-Cys9)

9

99.37%

C₃₅H₅₉N₁₃O₁₄S₂

950.05

Synthetic

Powder

The peptide CRGDKGPDC is a tumor-penetrating peptide that is used to deliver drugs into extravascular tumor tissue by increasing tumor vascular permeability through interaction with neuropilin (NRP). It is also known as iRGD, which is a prototypic tumor-penetrating CendR peptide. The peptide has been shown to inhibit spontaneous metastasis in mice and has a potent anti-metastatic effect. It works by binding to the NRP-1 receptor and inhibiting tumor cell migration and chemorepulsion. The peptide induces a collapse of cellular processes and partial cell detachment, resulting in the repellent activity. The anti-metastatic activity of iRGD may provide a significant additional benefit when this peptide is used for drug delivery to tumors.

Normally, this peptide will be delivered in lyophilized form and should be stored in a freezer at or below -20 °C. For more details, please refer to the manual: Handling and Storage of Synthetic Peptides

• Sugahara KN, Braun GB, de Mendoza TH, Kotamraju VR, French RP, Lowy AM, Teesalu T, Ruoslahti E. Tumor-penetrating iRGD peptide inhibits metastasis. Mol Cancer Ther. 2015 Jan;14(1):120-8. doi: 10.1158/1535-7163.MCT-14-0366. Epub 2014 Nov 12. PMID: 25392370; PMCID: PMC4297196.

Trifluoroacetic acid (TFA) has a significant impact on peptides due to its role in the peptide synthesis process.

TFA is essential for the protonation of peptides that lack basic amino acids such as Arginine (Arg), Histidine (His), and Lysine (Lys), or ones that have blocked N-termini. As a result, peptides often contain TFA salts in the final product.

TFA residues, when present in custom peptides, can cause unpredictable fluctuations in experimental data. At a nanomolar (nM) level, TFA can influence cell experiments, hindering cell growth at low concentrations (as low as 10 nM) and promoting it at higher doses (0.5–7.0 mM). It can also serve as an allosteric regulator on the GlyR of glycine receptors, thereby increasing receptor activity at lower glycine concentrations.

In an in vivo setting, TFA can trifluoroacetylate amino groups in proteins and phospholipids, inducing potentially unwanted antibody responses. Moreover, TFA can impact structure studies as it affects spectrum absorption.