| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
PEGs
PROTAC Linkers. |
|---|---|
| ln Vitro |
One ligand is for an E3 ubiquitin ligase, and the other is for the target protein; these two ligands are joined by a linker to form PROTACs. The intracellular ubiquitin-proteasome system is utilized by PROTACs to specifically destroy target proteins[1].
As a linker molecule, NH2-PEG3-C6-Cl itself has no intrinsic biological activity; it serves as a structural connector to join two essential ligands in a PROTAC molecule. Its role is to facilitate selective protein degradation by the ubiquitin-proteasome system, and its precise length and chemical composition are critical for optimal ternary complex formation and degradation efficacy. |
| ln Vivo |
No specific in vivo activity has been reported for this linker alone; its pharmacological activity is derived from the final PROTAC molecule after conjugation with appropriate ligands. The in vivo efficacy of a PROTAC is determined by the complete molecule and is measured in animal models.
|
| Enzyme Assay |
N/A; this compound is not assessed in enzyme/receptor binding assays. As a synthetic intermediate, its quality is typically confirmed by analytical methods such as HPLC (High-Performance Liquid Chromatography) and NMR (Nuclear Magnetic Resonance) spectroscopy, with a standard purity of 98%.
|
| Cell Assay |
N/A; this linker is not tested alone in cell-based assays. In a standard experimental protocol for a complete PROTAC, cells are treated with the compound for 4-24 hours. The readout for target engagement is typically a reduction in the protein of interest levels, as measured by Western blotting or a degradation assay.
|
| Animal Protocol |
N/A; no animal studies are performed with the linker alone. For a complete PROTAC conjugate, in vivo studies involve administering the compound to animal models and measuring plasma concentrations, target protein knockdown in tissues, and pharmacokinetic parameters.
|
| ADME/Pharmacokinetics |
The compound has a molecular weight of 267.79 and a molecular formula of C12H26ClNO3. It is typically stored as a powder at -20degC for up to 3 years, protected from light, or in a solvent at -80degC for 6 months or at -20degC for 1 month. It is soluble in DMSO (100 mg/mL).
|
| Toxicity/Toxicokinetics |
This product is for research use only and is not for human therapeutic or clinical applications. Standard chemical safety precautions should be observed during handling. The terminal amine and chloride groups allow for diverse conjugation chemistry to form PROTACs or other bioconjugates.
|
| References | |
| Additional Infomation |
This linker is widely used in bioconjugation, targeted drug delivery, surface functionalization, and the synthesis of multifunctional molecules for biomedical research. Its flexible PEG segment improves water solubility and reduces steric hindrance, making it a versatile reagent for constructing PROTAC libraries and various chemical biology probes.
|
| Molecular Formula |
C12H26CLNO3
|
|---|---|
| Molecular Weight |
267.792743206024
|
| Exact Mass |
267.16
|
| CAS # |
1261350-60-0
|
| PubChem CID |
127052438
|
| Appearance |
Colorless to light yellow liquid
|
| LogP |
0.9
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
14
|
| Heavy Atom Count |
17
|
| Complexity |
139
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C(N)COCCOCCOCCCCCCCl
|
| InChi Key |
RWQXYKFBNPVKHW-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C12H26ClNO3/c13-5-3-1-2-4-7-15-9-11-17-12-10-16-8-6-14/h1-12,14H2
|
| Chemical Name |
2-[2-[2-(6-chlorohexoxy)ethoxy]ethoxy]ethanamine
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| 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
|
|---|---|
| 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 | 3.7343 mL | 18.6713 mL | 37.3427 mL | |
| 5 mM | 0.7469 mL | 3.7343 mL | 7.4685 mL | |
| 10 mM | 0.3734 mL | 1.8671 mL | 3.7343 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
Copyright 2020 InvivoChem LLC | All Rights Reserved
