Certepetide (Synonyms: CEND-1; iRGD) |
| Catalog No.GC68856 |
Certepetide (CEND-1) is a novel tumor-targeting internalized arginine-glycine bifunctional cyclic peptide (a.k.a. iRGD), which is being developed for the treatment of solid tumors.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2580154-02-3
Sample solution is provided at 25 µL, 10mM.
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Certepetide (CEND-1) is a novel tumor-targeting internalized arginine-glycine bifunctional cyclic peptide (a.k.a. iRGD), which is being developed for the treatment of solid tumors[1]. Certepetide aims to overcome the existing challenges in the treatment of solid tumors by delivering combined anti-cancer drugs into tumors, selectively consuming immunosuppressive T cells, enhancing the killing ability of toxic T cells in the tumor microenvironment, and inhibiting the metastatic cascade reaction[2,3].
In vitro, when GFP-PC-3 and LM-PmC tumor cells were treated with Certepetide (10μM) for 24 hours, the random migration ability of LM-PmC and GFP-PC-3 cells in vitro was significantly inhibited, which was helpful in preventing the initial metastasis of tumor cells[2].
In vivo, Certepetide (4μmol/kg) was administered via tail vein injection in the mouse subcutaneous tumor model of liver cancer established by subcutaneous injection of HepG2 or Huh-7 cells (liver cancer cells). Certepetide can increase the concentration of sorafenib in subcutaneous tumor tissues without increasing systemic toxic effects. And enhance the killing ability of toxic T cells[4,5].
References:
[1]Winning A, Sietsema WK, Buck KK, Linsmeier A, Wiczling P. Population Pharmacokinetic Modeling of Certepetide in Human Subjects With Metastatic Pancreatic Ductal Adenocarcinoma. Clin Pharmacol Drug Dev. 2025 Mar;14(3):240-251.
[2] Sugahara KN, Teesalu T, Karmali PP, Kotamraju VR, Agemy L, Girard OM, Hanahan D, Mattrey RF, Ruoslahti E. Tissue-penetrating delivery of compounds and nanoparticles into tumors. Cancer Cell. 2009 Dec 8;16(6):510-20.
[3] Teesalu T, Sugahara KN, Kotamraju VR, Ruoslahti E. C-end rule peptides mediate neuropilin-1-dependent cell, vascular, and tissue penetration. Proc Natl Acad Sci U S A. 2009 Sep 22;106(38):16157-62.
[4] Schmithals C, Köberle V, Korkusuz H, Pleli T, Kakoschky B, Augusto EA, Ibrahim AA, Arencibia JM, Vafaizadeh V, Groner B, Korf HW, Kronenberger B, Zeuzem S, Vogl TJ, Waidmann O, Piiper A. Improving Drug Penetrability with iRGD Leverages the Therapeutic Response to Sorafenib and Doxorubicin in Hepatocellular Carcinoma. Cancer Res. 2015 Aug 1;75(15):3147-54.
[5] McEwen A., Henson C. Quantitative whole-body autoradiography: Past, present and future. Bioanalysis. 2015;7:557–568.
| Cell experiment [1]: | |
Cell lines | GFP-PC-3 cells; LM-PmC cells |
Preparation Method | Cell migration was analyzed using 24-well Transwell chambers containing polycarbonate membranes with 8-μm pores. Both sides of the membranes were coated with 50μg/ml of collagen type-I to facilitate initial cell attachment to the membranes. GFP-PC-3 (4 × 104 cells) or LM-PmC (2 × 105 cells) cells in DMEM containing 0.1% BSA were added to the upper compartment. The lower compartment was filled with 600μl of DMEM containing 0.1% BSA. Certepetide at a final concentration of 10μM or PBS were added to both the upper and lower compartments. The total number of cells that migrated to the lower side of the membranes was determined by counting cell numbers under low magnification. |
Reaction Conditions | 10μM; 24h |
Applications | Certepetide can inhibit the in vitro random migration ability of LM-PmC and GFP-PC-3 tumor cells, which is helpful in preventing the initial metastasis of tumor cells. |
| Animal experiment [2]: | |
Animal models | Nude mice |
Preparation Method | A total of 5 × 106 HepG2 or Huh-7 cells (resuspended in 100μL of PBS) was injected subcutaneously into nude mice. Three to 4 weeks later, the mice were assigned to the treatment groups. Doxorubicin was dissolved in PBS and sorafenib in a vehicle containing 12.5% Cremophor and 12.5% ethanol. Nude mice bearing HepG2 or Huh-7 xenografts received Certepetide (4μmol/kg by tail vein injection), or PBS 15 minutes each time before treatment with doxorubicin (3mg/kg, 3 times per week intraperitoneally) or sorafenib (every second day orally). Body weight and tumor size were determined every 2 to 3 days with a caliper. At the end of the experiment, the mice were sacrificed by cervical dislocation. Tumors were excised and weighed. |
Dosage form | 4μmol/kg; 28 days; i.v. |
Applications | Certepetide can increase the concentration of sorafenib in subcutaneous tumor tissues without increasing systemic toxic effects and enhancing the killing ability of toxic T cells |
References: | |
| Cas No. | 2580154-02-3 | SDF | |
| Synonyms | CEND-1; iRGD | ||
| Formula | C37H60N14O14S2 | M.Wt | 989.09 |
| Solubility | Storage | Store at -20°C | |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.011 mL | 5.0552 mL | 10.1103 mL |
| 5 mM | 202.2 μL | 1.011 mL | 2.0221 mL |
| 10 mM | 101.1 μL | 505.5 μL | 1.011 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
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