Certepetide
Based on 1 publication(s) in Google Scholar
Certepetide (CEND-1) is a bifunctional cyclic peptide (a.k.a. iRGD). Certepetide is a tumor-penetrating enhancer via RGD motif interaction with alphav-integrins and via activating NRP-1, and transforms the solid tumor microenvironment into a temporary agent conduit. Certepetide accumulates in tumors, and is used in the research of pancreatic cancer and other solid tumors.
For research use only. We do not sell to patients.
- Purity : 99.80%
- CAS No.: 2580154-02-3
- Formula: C37H60N14O14S2
- Molecular Weight:989.09
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Storage:
Sealed storage, away from moisture and light, under nitrogen.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Certepetide
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Biological Activity
Description
IC50 & Target
Alphav-integrins, NRP-1[3].
In Vivo
CEND-1 enhances the penetration of anticancer therapeutics specifically into tumours, but not into normal tissues, it also holds the potential for dose reductions, which can attenuate side effects[4].
CEND-1 (intravenously injected) increases the levels of co-administered Evans blue approximately threefold[5].
| Table 1. Derived mean pharmacokinetic parameters for CEND-1 in mouse, rat, dog and monkey plasma after a single intravenous infusion of CEND-1 (±SD) [5]. | ||||||||||||||||||||||||||||||||||||
| Number of Animals (Sex) | CEND-1 Dose (mg/kg) | t1/2 (h) | C0 (ng/mL) | V (mL/kg) | Cl_obs (mL/hr/kg) | AUC0-inf (h*ng/mL) | ||||||||||||||||||||||||||||||
| Mouse * | ||||||||||||||||||||||||||||||||||||
| 3 (M) | 1.5 | 0.306 | 10,343 | 449 | 1016 | 1476 | ||||||||||||||||||||||||||||||
| 3 (M) | 13.5 | 0.547 | 68,358 | 1007 | 1277 | 10,569 | ||||||||||||||||||||||||||||||
| Rat* | ||||||||||||||||||||||||||||||||||||
| 6 (M) | 75 | 0.341 | 469,000 | 171 | 348 | 215,476 | ||||||||||||||||||||||||||||||
| 6 (F) | 75 | 0.391 | 436,333 | 254 | 451 | 166,331 | ||||||||||||||||||||||||||||||
| Dog* | ||||||||||||||||||||||||||||||||||||
| 3 (M) | 1 | 0.665 (0.0448) | 6010 (1985) | 241 (27) | 253 (40.1) | 4030 (686) | ||||||||||||||||||||||||||||||
| 3 (F) | 5 | 0.648 (0.0486) | 25,133 (3635) | 230 (14.6) | 247 (32.9) | 20,443 (2530) | ||||||||||||||||||||||||||||||
| Monkey* | ||||||||||||||||||||||||||||||||||||
| 3 (M) | 5 | 0.888 (0.0963) | 55,082 (19,905) | 204 (14.1) | 179 (23.4) | 28,230 (3865) | ||||||||||||||||||||||||||||||
| 3 (M) | 50 | 0.956 (0.0869) | 602,161 (211,386) | 162 (32.1) | 178 (51.9) | 421,119 (171,418) | ||||||||||||||||||||||||||||||
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2580154-02-3
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Appearance Solid
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Molecular Weight 989.09
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Formula C37H60N14O14S2
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Color White to off-white
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Synonyms
CEND-1; iRGD; LSTA1
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Sequence Shortening
Ac-CRGDKGPDC-NH2 (Disulfide bridge: Cys1-Cys9)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture and light, under nitrogen
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
In Vitro:
H2O : ≥ 50 mg/mL (50.55 mM)
DMSO : 2.33 mg/mL (2.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Multiplex immunofluorescence IHC
Multiplex immunofluorescence IHC detects multiple protein biomarkers in one tissue section by sequential antibody staining, HRP-mediated tyramide fluorophore deposition, heat-mediated antibody stripping, nuclear counterstaining, multispectral imaging, spectral unmixing, and digital cell phenotyping; TSA deposits fluorophore near the antigen so the fluorescence signal remains after primary and secondary antibodies are removed, enabling repeated staining cycles, including with antibodies from the same host species. Classic FFPE tumor immune-profiling applications use panels such as CD3, CD8, CD68/CD163, FOXP3, PD-1, PD-L1, pancytokeratin, Ki67, and DAPI to identify tumor cells, immune-cell subsets, checkpoint-marker expression, co-expression phenotypes, cell density, and spatial relationships in the tumor microenvironment.
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Multiplex immunohistochemistry
Multiplex immunohistochemistry (mIHC), also known as tyramide dignal amplification (TSA), is an enzymatic detection method that uses horseradish peroxidase (HRP) to perform high-density in-situ labeling of target proteins or nucleic acids.
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Research Protocol for Cancer Immunology
Cancer immunology studies how the immune system recognizes, suppresses, edits, or fails to eliminate malignant cells through tumor antigen release, antigen presentation, T-cell priming, immune trafficking, tumor-cell killing, and feedback inhibition in the tumor microenvironment. The cancer-immunity cycle links tumor antigenicity, dendritic-cell priming, CD8+ T-cell infiltration, cytotoxic function, and immune-checkpoint regulation to tumor rejection or immune escape. Immune-checkpoint pathways such as PD-1/PD-L1 and CTLA-4 suppress antitumor T-cell activity and can be therapeutically blocked, but many tumors remain resistant because of poor antigen presentation, weak T-cell infiltration, suppressive myeloid cells, regulatory T cells, and tumor-intrinsic immune-exclusion programs. Unresolved questions include which immune-cell states predict response, how tumor-intrinsic pathways exclude immune cells, how myeloid suppression limits checkpoint blockade, and which combination strategies
Purity & Documentation
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Data Sheet (288 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[2]. Ruoslahti Erkki, et al. Methods for treating pancreatic cancer and other solid tumors. WO2021226148.
[4]. Harri A Järveläinen, et al. Assessment of the Pharmacokinetics, Disposition, and Duration of Action of the Tumour-Targeting Peptide CEND-1. Int J Mol Sci. 2023 Mar 16;24(6):5700. [Content Brief]
[5]. Schmithals, C, et al. 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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 1.0110 mL | 5.0552 mL | 10.1103 mL | 25.2758 mL |
| H2O | 5 mM | 0.2022 mL | 1.0110 mL | 2.0221 mL | 5.0552 mL |
| 10 mM | 0.1011 mL | 0.5055 mL | 1.0110 mL | 2.5276 mL | |
| 15 mM | 0.0674 mL | 0.3370 mL | 0.6740 mL | 1.6851 mL | |
| 20 mM | 0.0506 mL | 0.2528 mL | 0.5055 mL | 1.2638 mL | |
| 25 mM | 0.0404 mL | 0.2022 mL | 0.4044 mL | 1.0110 mL | |
| 30 mM | 0.0337 mL | 0.1685 mL | 0.3370 mL | 0.8425 mL | |
| 40 mM | 0.0253 mL | 0.1264 mL | 0.2528 mL | 0.6319 mL | |
| 50 mM | 0.0202 mL | 0.1011 mL | 0.2022 mL | 0.5055 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Certepetide Related Classifications
HY-P3448 Related Classifications
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