| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
Certepetide targets alphav integrins (alphavbeta3/5) expressed on tumor endothelium via its RGD motif. After binding and proteolytic cleavage, the resulting fragment activates neuropilin-1 (NRP-1), triggering active, tumor-specific, and non-invasive drug transport into tumor cells, thereby enhancing drug penetration.
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| ln Vitro |
In cell-free binding assays, Certepetide binds to purified alphavbeta3 integrin with high affinity. The RGD motif is critical for this interaction. In co-culture models of endothelial and cancer cells, Certepetide facilitates the trans-endothelial transport of co-administered small molecule chemotherapeutics (e.g., doxorubicin, paclitaxel) and nanoparticles without increasing systemic toxicity.
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| ln Vivo |
Certepetide accumulates in tumors and enhances the penetration and efficacy of co-administered anticancer drugs in various mouse xenograft models of pancreatic cancer and other solid tumors. It has been shown to significantly improve survival when combined with standard-of-care chemotherapy, without causing off-target toxicity.
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| Enzyme Assay |
This cell-free binding assay is performed using purified recombinant alphavbeta3 integrin protein. The protein is immobilized on a 96-well plate. Certepetide (1 nM - 100 uM) is added and incubated for 1-2 hours. Binding is detected using an anti-Certepetide antibody and HRP-conjugated secondary antibody, or by surface plasmon resonance (SPR) to calculate the Kd.
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| Cell Assay |
Human endothelial cells (e.g., HUVECs) and cancer cells are co-cultured in a transwell system to model the tumor vessel barrier. Certepetide (1-100 uM) and a fluorescently labeled chemotherapy drug (e.g., doxorubicin) are added to the upper chamber. Drug penetration into the lower chamber (cancer cells) is quantified by fluorescence microscopy or flow cytometry after 1-4 hours.
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| Animal Protocol |
In a murine pancreatic cancer xenograft model (e.g., subcutaneous or orthotopic), Certepetide is co-administered with standard-of-care chemotherapy (e.g., gemcitabine + nab-paclitaxel). The cyclic peptide is administered intravenously (IV) at 1-10 mg/kg, typically 10-30 minutes before chemotherapy. Tumor volume is measured by calipers; tumor drug levels are measured by HPLC-MS; survival is monitored.
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| ADME/Pharmacokinetics |
PK studies in rodents show Certepetide has a short half-life (approximately 10-20 minutes) due to rapid proteolytic degradation. It is rapidly cleared from the circulation but accumulates in tumors for up to 24 hours. This brief plasma exposure is sufficient to trigger tumor-selective permeability, leading to enhanced drug delivery. Good aqueous solubility (>10 mg/mL).
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| Toxicity/Toxicokinetics |
Toxicology studies in preclinical models indicate that Certepetide is well-tolerated, with no significant adverse events at therapeutic doses. It does not increase the toxicity profile of co-administered chemotherapy drugs. It is not immunogenic. Standard safety precautions for peptides and research chemicals apply.
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| References | |
| Additional Infomation |
Certepetide (also known as CEND-1, iRGD, LSTA1) is an investigational drug. It has received FDA Fast Track and Orphan Drug designations for pancreatic cancer. It has been evaluated in phase 1/2 clinical trials for solid tumors, demonstrating safety and encouraging signals of efficacy when combined with chemotherapy. Not yet approved.
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| Molecular Formula |
C37H60N14O14S2
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|---|---|
| Molecular Weight |
989.09
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| Exact Mass |
988.385
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| CAS # |
2580154-02-3
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| PubChem CID |
164886680
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| Appearance |
White to off-white solid powder
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| LogP |
-9.4
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| Hydrogen Bond Donor Count |
14
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| Hydrogen Bond Acceptor Count |
18
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
67
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| Complexity |
1870
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| Defined Atom Stereocenter Count |
7
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| SMILES |
S1C([H])([H])[C@@]([H])(C(N([H])[H])=O)N([H])C([C@]([H])(C([H])([H])C(=O)O[H])N([H])C([C@]2([H])C([H])([H])C([H])([H])C([H])([H])N2C(C([H])([H])N([H])C([C@]([H])(C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])[H])N([H])C([C@]([H])(C([H])([H])C(=O)O[H])N([H])C(C([H])([H])N([H])C([C@]([H])(C([H])([H])C([H])([H])C([H])([H])/N=C(\N([H])[H])/N([H])[H])N([H])C([C@]([H])(C([H])([H])S1)N([H])C(C([H])([H])[H])=O)=O)=O)=O)=O)=O)=O)=O)=O
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| InChi Key |
YPHPUVJQSYACEN-HUVRVWIJSA-N
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| InChi Code |
InChI=1S/C37H60N14O14S2/c1-18(52)45-24-17-67-66-16-23(30(39)59)50-34(63)22(13-29(57)58)49-36(65)25-8-5-11-51(25)27(54)15-44-32(61)19(6-2-3-9-38)47-33(62)21(12-28(55)56)46-26(53)14-43-31(60)20(48-35(24)64)7-4-10-42-37(40)41/h19-25H,2-17,38H2,1H3,(H2,39,59)(H,43,60)(H,44,61)(H,45,52)(H,46,53)(H,47,62)(H,48,64)(H,49,65)(H,50,63)(H,55,56)(H,57,58)(H4,40,41,42)/t19-,20-,21-,22-,23-,24-,25-/m0/s1
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| Chemical Name |
2-[(6S,9S,15S,18R,23R,26S,29S)-18-acetamido-6-(4-aminobutyl)-23-carbamoyl-26-(carboxymethyl)-15-[3-(diaminomethylideneamino)propyl]-2,5,8,11,14,17,25,28-octaoxo-20,21-dithia-1,4,7,10,13,16,24,27-octazabicyclo[27.3.0]dotriacontan-9-yl]acetic acid
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 1.0110 mL | 5.0552 mL | 10.1103 mL | |
| 5 mM | 0.2022 mL | 1.0110 mL | 2.0221 mL | |
| 10 mM | 0.1011 mL | 0.5055 mL | 1.0110 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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