Mal-PEG6-PFP is a non-cleavable PEG Linker used in the synthesis of ADC. It is composed of a Maleimide group, 4-unit PEG and a PFP ester.
Physicochemical Properties
| Molecular Formula | C25H30F5NO10 |
| Molecular Weight | 599.498425960541 |
| Exact Mass | 599.179 |
| CAS # | 1599486-33-5 |
| PubChem CID | 77078505 |
| Appearance | Typically exists as solid at room temperature |
| Density | 1.4±0.1 g/cm3 |
| Boiling Point | 623.0±55.0 °C at 760 mmHg |
| Flash Point | 330.6±31.5 °C |
| Vapour Pressure | 0.0±1.8 mmHg at 25°C |
| Index of Refraction | 1.490 |
| LogP | 0.57 |
| Hydrogen Bond Donor Count | 0 |
| Hydrogen Bond Acceptor Count | 15 |
| Rotatable Bond Count | 23 |
| Heavy Atom Count | 41 |
| Complexity | 792 |
| Defined Atom Stereocenter Count | 0 |
| SMILES | FC1C(=C(C(=C(C=1OC(CCOCCOCCOCCOCCOCCOCCN1C(C=CC1=O)=O)=O)F)F)F)F |
| InChi Key | HDNANNZNASDAGQ-UHFFFAOYSA-N |
| InChi Code | InChI=1S/C25H30F5NO10/c26-20-21(27)23(29)25(24(30)22(20)28)41-19(34)3-5-35-7-9-37-11-13-39-15-16-40-14-12-38-10-8-36-6-4-31-17(32)1-2-18(31)33/h1-2H,3-16H2 |
| Chemical Name | (2,3,4,5,6-pentafluorophenyl) 3-[2-[2-[2-[2-[2-[2-(2,5-dioxopyrrol-1-yl)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoate |
| 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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| 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]. |
| References |
[1]. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562. |
Solubility Data
| Solubility (In Vitro) | DMSO : ~100 mg/mL (~166.81 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.17 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6681 mL | 8.3403 mL | 16.6806 mL | |
| 5 mM | 0.3336 mL | 1.6681 mL | 3.3361 mL | |
| 10 mM | 0.1668 mL | 0.8340 mL | 1.6681 mL |