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| 1mg |
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| 10mg |
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| Targets |
iRGD peptide 1 TFA targets two distinct molecules: first, integrin alphavbeta3 and alphavbeta5 via the RGD motif; second, neuropilin-1 (NRP-1) after proteolytic cleavage exposes the CendR motif (R/KXXR/K). Binding to integrins mediates initial tumor homing, while NRP-1 binding triggers endocytosis and transcytosis, facilitating deep tumor penetration.
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| ln Vitro |
In vitro, iRGD peptide 1 (iRGD) causes chemorepulsion and inhibits tumor cell migration in a way that is dependent on CendR and NRP-1. The repelling action of iRGD peptide 1 is caused by a severe breakdown of cellular processes and partial cell separation. When the cells are seeded on fibronectin, these changes are clearly visible, indicating a role for CendR in the functional control of integrins[1].
In cell-free binding assays, iRGD binds to purified alphavbeta3 integrin with a Kd in the sub-micromolar range (SPR). The cleaved CendR motif (CRGDK/R) binds to neuropilin-1 (b1 domain) with a Kd around 1-10 uM. The cyclic structure is essential for integrin binding; linear iRGD has reduced activity. Binding is not enzymatic; it is a protein-peptide interaction. |
| ln Vivo |
iRGD peptide 1 administered intravenously every other day for 21 days at a dose of 4 μmol/kg (amino acid sequence: CRGDKGPDC) significantly prevents mice from developing spontaneous metastases[1].
In cell culture, iRGD (10-100 uM) enhances the uptake and penetration of co-administered small molecules, nanoparticles, or antibodies into 3D tumor spheroids. The peptide itself does not have direct cytotoxic activity. When conjugated to or co-injected with chemotherapeutics (e.g., doxorubicin), iRGD increases their anti-tumor efficacy. The effect is blocked by anti-NRP-1 antibodies or CendR antagonists. |
| Enzyme Assay |
Integrin binding is measured by a cell-free ELISA: 96-well plates coated with alphavbeta3 integrin are incubated with biotinylated iRGD in the presence or absence of excess unlabeled iRGD. Bound iRGD is detected with streptavidin-HRP. For NRP-1 binding, surface plasmon resonance is used: recombinant NRP-1 b1 domain is immobilized, and iRGD or its cleaved form is injected. Kinetic parameters (Kd) are calculated.
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| Cell Assay |
For spheroid penetration assays, cancer cells (e.g., U87MG, MDA-MB-231) are cultured in ultralow attachment plates to form spheroids. Spheroids are incubated with fluorescently labeled iRGD (1-100 uM) plus a fluorescent cargo (e.g., 40 kDa dextran) for 2-24 hours. Penetration depth is measured by confocal microscopy. The effect of iRGD is compared to a control peptide (RAD) or NRP-1 blocking antibody. Co-incubation with the peptide increases cargo penetration into the spheroid core.
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| Animal Protocol |
iRGD peptide 1 TFA is evaluated in mouse xenograft models (e.g., pancreatic, breast, or prostate cancer). The peptide (1-10 mg/kg) is co-administered intravenously with a chemotherapeutic agent or a nanomedicine. Treatment is given every 2-3 days for 2-4 weeks. Tumor volume and drug accumulation (by tissue fluorescence or LC-MS/MS) are measured. iRGD significantly increases drug concentrations within tumors (2-10-fold) and improves anti-tumor efficacy compared to drug alone. No major toxicity is reported.
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| ADME/Pharmacokinetics |
iRGD has a short plasma half-life (minutes to 1 hour) due to rapid proteolysis and renal clearance. It is administered intravenously (bolus or infusion) to achieve peak concentrations during the window of drug delivery. The peptide is soluble in PBS (TFA salt). When conjugated to nanoparticles, the PK properties are governed by the carrier. For co-administration, iRGD is injected immediately before or together with the cargo to maximize the penetration effect.
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| Toxicity/Toxicokinetics |
iRGD is well-tolerated in mice at doses up to 20 mg/kg. No significant body weight loss, organ toxicity, or hemolysis has been observed. Off-target effects are minimal because the peptide relies on tumor-specific integrin expression. At high doses, mild hypotension or flushing may occur due to NRP-1 activation in endothelial cells. The TFA counterion is present at safe levels. No clinical toxicity data are available.
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| References |
[1]. Kazuki N Sugahara, et al. Tumor-penetrating iRGD Peptide Inhibits Metastasis. Mol Cancer Ther. 2015 Jan;14(1):120-8.
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| Additional Infomation |
iRGD is a research peptide widely used to enhance drug delivery to solid tumors. It has been tested in preclinical models and has entered phase I clinical trials (e.g., with co-administered drugs). As of now, iRGD itself is not an approved drug; it is used as a targeting and penetration enhancer. The TFA salt form improves solubility. The peptide sequence is cyclic via disulfide bridge between cysteines. Not for human therapeutic use outside clinical trials.
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| Molecular Formula |
C37H60F3N13O16S2
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| Molecular Weight |
1064.08
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| Appearance |
Typically exists as solid at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O :~100 mg/mL (~93.98 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9398 mL | 4.6989 mL | 9.3978 mL | |
| 5 mM | 0.1880 mL | 0.9398 mL | 1.8796 mL | |
| 10 mM | 0.0940 mL | 0.4699 mL | 0.9398 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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