| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
CRBN (cereblon), an E3 ubiquitin ligase.
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| 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 4'-PEG2-azide itself has no intrinsic biological activity; its function is to recruit the E3 ubiquitin ligase complex. The azide group enables copper-catalyzed azide-alkyne cycloaddition (CuAAC) or strain-promoted azide-alkyne cycloaddition (SPAAC) with alkyne-containing molecules for PROTAC synthesis. |
| 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.
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| Enzyme Assay |
N/A; as a synthetic intermediate, its quality is confirmed by analytical methods such as HPLC and NMR, with a standard purity of ≥95%. The azide group is a bioorthogonal handle that can react with alkyne groups under click chemistry conditions.
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| Cell Assay |
N/A; this conjugate is not tested alone in cell-based assays but is used as a building block for constructing PROTACs. In a typical click chemistry protocol, the azide group reacts with an alkyne-containing ligand in the presence of a copper catalyst (e.g., CuSO4 and sodium ascorbate) to form a stable 1,2,3-triazole linkage.
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| 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 via intraperitoneal (IP) or intravenous (IV) injection.
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| ADME/Pharmacokinetics |
This compound has a molecular weight of 430.42, a molecular formula of C19H22N6O6, and is stored as a solid at -20degC. It is soluble in DMSO. The product is part of a range of functionalized tool molecules for PROTAC R&D and requires protection from light during transportation and storage.
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| Toxicity/Toxicokinetics |
This product is for research use only and is not for human or veterinary use. Standard chemical safety precautions should be followed during handling. PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
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| References | |
| Additional Infomation |
The terminal azide 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.
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| Molecular Formula |
C19H22N6O6
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|---|---|
| Molecular Weight |
430.414583683014
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| Exact Mass |
430.16
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| CAS # |
2271036-45-2
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| PubChem CID |
137321407
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| Appearance |
White to yellow solid powder
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| LogP |
1.5
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
31
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| Complexity |
754
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CC(=O)NC(=O)C1N2C(=O)C3=C(C2=O)C(=CC=C3)NCCOCCOCCN=[N+]=[N-]
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| InChi Key |
BBYXCRBBKSBKOA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H22N6O6/c20-24-22-7-9-31-11-10-30-8-6-21-13-3-1-2-12-16(13)19(29)25(18(12)28)14-4-5-15(26)23-17(14)27/h1-3,14,21H,4-11H2,(H,23,26,27)
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| Chemical Name |
4-[2-[2-(2-azidoethoxy)ethoxy]ethylamino]-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione
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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 | 2.3234 mL | 11.6168 mL | 23.2337 mL | |
| 5 mM | 0.4647 mL | 2.3234 mL | 4.6467 mL | |
| 10 mM | 0.2323 mL | 1.1617 mL | 2.3234 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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