Certepetide
Based on 1 Customer Validation
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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Alphav-integrins, NRP-1[3].
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.
| 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)
Solvent & Solubility
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)
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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