| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Cereblon
CRBN (Cereblon), an E3 ubiquitin ligase. |
|---|---|
| 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 cereblon-binding ligand-linker conjugate, Pomalidomide-PEG2-azide itself has no intrinsic biological activity; its function is to recruit the E3 ubiquitin ligase complex. It is the final PROTAC molecule, created by conjugating this building block to a target protein ligand via click chemistry, that will bind to a target protein and facilitate its ubiquitination and subsequent proteasomal degradation. |
| ln Vivo |
No specific in vivo activity has been reported for this conjugate alone; its in vivo degradation activity is observed only when conjugated to a target protein ligand to form a complete PROTAC molecule. The in vivo efficacy of a PROTAC is typically evaluated in mouse xenograft models of target-driven cancers.
|
| Enzyme Assay |
N/A; this compound is not assessed in isolated enzyme/receptor binding assays. Its cereblon-binding affinity can be validated via biophysical methods such as surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) as part of a complete PROTAC construct. The azide group is a bioorthogonal handle that can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAC) or strain-promoted azide-alkyne cycloaddition (SPAAC) with alkyne-containing molecules.
|
| Cell Assay |
N/A; this conjugate alone is not tested in cell-based assays but is used as a building block for constructing PROTACs. In a typical cellular assay, a complete PROTAC synthesized from this conjugate is incubated with target-expressing cancer cells for 4-24 hours, after which target protein levels are measured by Western blotting to determine the DC50 (half-maximal degradation concentration).
|
| Animal Protocol |
N/A; no animal studies are performed with the ligand-linker conjugate alone. For in vivo studies, the complete PROTAC molecule is typically formulated in a vehicle such as 10% DMSO, 40% PEG300, 5% Tween-80, and 45% saline, and administered to tumor-bearing mice via intraperitoneal (IP) or intravenous (IV) injection. Efficacy is measured by tumor growth inhibition (TGI) and target protein knockdown in tumor tissues.
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| ADME/Pharmacokinetics |
This compound has a molecular weight of 444.40. It is typically stored as a powder at -20degC for up to 3 years or in a solvent at -80degC for up to 1 year. It is soluble in DMSO and is stable under recommended storage conditions. The azide functional group allows for versatile conjugation via click chemistry.
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| Toxicity/Toxicokinetics |
This product is for research use only and is not intended for human or veterinary use. Standard safe handling practices for laboratory chemical reagents should be followed. PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.
|
| References | |
| Additional Infomation |
The terminal azide (N3) group enables bioorthogonal conjugation, allowing for the mild and selective attachment of the cereblon ligand to alkyne-functionalized target protein ligands. This click chemistry approach facilitates the parallel synthesis of PROTAC libraries to screen for optimal linkers and ligands for efficient ternary complex formation and target degradation.
|
| Molecular Formula |
C19H20N6O7
|
|---|---|
| Molecular Weight |
444.398103713989
|
| Exact Mass |
444.139
|
| CAS # |
2267306-14-7
|
| PubChem CID |
155292127
|
| Appearance |
Off-white to light yellow solid powder
|
| LogP |
0.5
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
32
|
| Complexity |
827
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1CC(=O)NC(=O)C1N2C(=O)C3=C(C2=O)C(=CC=C3)NC(=O)COCCOCCN=[N+]=[N-]
|
| InChi Key |
QMQAWNMGKYQDLT-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H20N6O7/c20-24-21-6-7-31-8-9-32-10-15(27)22-12-3-1-2-11-16(12)19(30)25(18(11)29)13-4-5-14(26)23-17(13)28/h1-3,13H,4-10H2,(H,22,27)(H,23,26,28)
|
| Chemical Name |
2-[2-(2-azidoethoxy)ethoxy]-N-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]acetamide
|
| 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) |
DMSO :~90 mg/mL (~202.52 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (11.25 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2502 mL | 11.2511 mL | 22.5023 mL | |
| 5 mM | 0.4500 mL | 2.2502 mL | 4.5005 mL | |
| 10 mM | 0.2250 mL | 1.1251 mL | 2.2502 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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