| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
PEGs
The DOTA group chelates di- and trivalent cations (including radiometals 64Cu, 68Ga, 177Lu, etc.); DBCO enables copper-free click chemistry with azides. No biological target. |
|---|---|
| ln Vitro |
A linker separates the two ligands that make up PROTACs; one ligand is for an E3 ubiquitin ligase, and the other is for the target protein. Target proteins are selectively degraded by PROTACs by taking advantage of the intracellular ubiquitin-proteasome system[1].
DOTA-PEG5-C6-DBCO has no direct biological activity; the DOTA moiety forms stable coordination complexes with diagnostic and therapeutic radionuclides for PET imaging or radiotherapy; the DBCO group enables SPAAC. |
| ln Vivo |
No direct in vivo activity; radiolabeled conjugates prepared using DOTA-PEG5-C6-DBCO can be used for in vivo tumor imaging (PET/SPECT) and targeted radiotherapy in animal models.
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| Enzyme Assay |
Labeling efficiency assessed by radiolabeling with 64Cu, 68Ga, or 177Lu; chelation efficiency measured by ITLC or HPLC; click conjugation efficiency with azide-modified biomolecules assessed by HPLC or mass spectrometry.
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| Cell Assay |
Not applicable; cells are incubated with radiolabeled conjugates prepared using DOTA-PEG5-C6-DBCO to assess cellular uptake and binding; cell-associated radioactivity measured by gamma counter.
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| Animal Protocol |
Mice bearing tumor xenografts receive 68Ga- or 177Lu-labeled DOTA-PEG5-C6-DBCO conjugates (50-200 microCi, IV); PET/CT or SPECT/CT imaging is performed at various time points; biodistribution assessed by ex vivo organ counting.
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| ADME/Pharmacokinetics |
No PK data for the linker itself; radiolabeled conjugates prepared from DOTA-PEG5-C6-DBCO show typical PK behavior of peptide/antibody conjugates with PEGylation improving circulation time.
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| Toxicity/Toxicokinetics |
As a chelator-linker, DOTA-PEG5-C6-DBCO has low inherent toxicity; potential toxicity depends on the radiometal or cargo conjugated; standard safety precautions required for handling radiometals.
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| References | |
| Additional Infomation |
DOTA-PEG5-C6-DBCO is a research-grade chemical tool for radiolabeling and bioconjugation; not a drug; no clinical trial or marketing approval status; for research use only.
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| Molecular Formula |
C49H71N7O14
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|---|---|
| Molecular Weight |
982.13
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| Appearance |
White to off-white solid powder
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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 |
| 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) |
DMSO :~125 mg/mL (~127.27 mM)
H2O :~125 mg/mL (~127.27 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 | 1.0182 mL | 5.0910 mL | 10.1820 mL | |
| 5 mM | 0.2036 mL | 1.0182 mL | 2.0364 mL | |
| 10 mM | 0.1018 mL | 0.5091 mL | 1.0182 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.
Products are for research use only; We do not sell to patients
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