| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Azido-PEG4-PFP ester itself does not bind to a specific biological target. The PFP ester group reacts with primary amines (-NH2) to form stable amide bonds. The PFP ester is more hydrolytically stable than NHS esters. The azide group enables click chemistry reactions. As a PROTAC linker, it joins an E3 ubiquitin ligase ligand to a target protein ligand.
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|---|---|
| ln Vitro |
In vitro activity is primarily related to its function as a linker. It enables the formation of stable conjugates via amide bond formation and click chemistry. The PFP ester provides superior hydrolytic stability compared to NHS esters. PROTACs synthesized using this linker facilitate targeted protein degradation. No direct pharmacological activity is attributed to the linker itself.
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| ln Vivo |
In vivo activity is inferred from the performance of PROTACs or conjugates synthesized using this linker. PROTACs incorporating PEG-based linkers can induce targeted protein degradation in vivo. The PEG spacer improves pharmacokinetic properties by increasing solubility. No direct in vivo activity is associated with the linker alone.
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| Enzyme Assay |
In vitro assays for Azido-PEG4-PFP ester typically involve evaluating the efficiency of conjugation. The PFP ester is reacted with primary amine-containing molecules. The azide group is reacted with alkyne-containing molecules via click chemistry. Reaction progress is monitored by HPLC, mass spectrometry, or ¹⁹F NMR. Purity is assessed by HPLC. Hydrolytic stability is compared to NHS ester linkers.
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| Cell Assay |
Cell-based assays for Azido-PEG4-PFP ester are conducted in the context of the final PROTAC or conjugate molecule. Cells are treated with the conjugate and evaluated for target-specific protein degradation (for PROTACs). Cytotoxicity is measured by MTT or CellTiter-Glo assays. Target engagement is evaluated by cellular thermal shift assay (CETSA) or NanoBRET.
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| Animal Protocol |
In vivo animal studies are performed with PROTACs or conjugates containing this linker. Tumor-bearing mice are treated with the conjugate, and tumor growth inhibition is monitored. Pharmacokinetic parameters are evaluated by measuring conjugate levels in blood and tissues. Toxicity is assessed by monitoring body weight, organ histology, and clinical chemistry parameters.
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| ADME/Pharmacokinetics |
Azido-PEG4-PFP ester (molecular weight ~500, formula C21H27F5N4O7) is a PEG-based linker. The PFP ester provides superior hydrolytic stability compared to NHS esters. The azide group enables click chemistry. No specific PK data are available for this linker alone; its PK profile is determined by the conjugated molecule.
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| Toxicity/Toxicokinetics |
No detailed toxicology data are specifically available for Azido-PEG4-PFP ester. The pentafluorophenyl group may present additional toxicity considerations. The compound is for research use only and not intended for therapeutic use. Standard laboratory safety precautions should be followed. Store at -20°C.
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| Additional Infomation |
Azido-PEG4-PFP ester (CAS#: 1353012-00-6) is a PEG-based linker containing an azide group and a pentafluorophenyl (PFP) ester. The PFP ester demonstrates superior hydrolytic stability relative to NHS ester-based linkers. Molecular weight: ~500, formula: C21H27F5N4O7.
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| Molecular Formula |
C17H20F5N3O6
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|---|---|
| Molecular Weight |
457.3492
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| Exact Mass |
457.127
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| CAS # |
1353012-00-6
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| PubChem CID |
60146185
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| Appearance |
Colorless to light yellow liquid
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| LogP |
1.67
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
17
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| Heavy Atom Count |
31
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| Complexity |
544
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C(=C(C(=C(C=1OC(C([H])([H])C([H])([H])OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])N=[N+]=[N-])=O)F)F)F)F
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| InChi Key |
QSIFGTAWLLFXPY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H20F5N3O6/c18-12-13(19)15(21)17(16(22)14(12)20)31-11(26)1-3-27-5-7-29-9-10-30-8-6-28-4-2-24-25-23/h1-10H2
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| Chemical Name |
(2,3,4,5,6-pentafluorophenyl) 3-[2-[2-[2-(2-azidoethoxy)ethoxy]ethoxy]ethoxy]propanoate
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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) |
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 | 2.1865 mL | 10.9325 mL | 21.8651 mL | |
| 5 mM | 0.4373 mL | 2.1865 mL | 4.3730 mL | |
| 10 mM | 0.2187 mL | 1.0933 mL | 2.1865 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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