| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
Pomalidomide-5-C12-NH2 hydrochloride targets the E3 ubiquitin ligase cereblon (CRBN) by binding to it via its Pomalidomide moiety. It is a CRBN ligand that facilitates the recruitment of the CRBN protein. It is a Pomalidomide-derived cereblon (CRBN) ligand. This compound is a valuable building block for the development of selective degraders in oncology.
|
|---|---|
| ln Vitro |
The primary in vitro activity of Pomalidomide-5-C12-NH2 hydrochloride is its ability to bind to the E3 ubiquitin ligase cereblon (CRBN). It is a Pomalidomide-derived cereblon ligand. It can be conjugated to a protein-targeting ligand via a linker to create a PROTAC. The resulting PROTAC can then induce the ubiquitination and degradation of the target protein.
|
| ln Vivo |
Pomalidomide-5-C12-NH2 hydrochloride is a building block for PROTACs, which are used in vivo to degrade target proteins. By recruiting CRBN, a PROTAC containing this ligand can lead to the targeted degradation of an oncogenic protein in an animal model. It is a valuable intermediate for developing selective degraders in oncology.
|
| Enzyme Assay |
A cell-free binding assay for Pomalidomide-5-C12-NH2 hydrochloride would involve SPR or a TR-FRET-based competition binding assay to measure its affinity for recombinant cereblon (CRBN) protein. The compound is dissolved in DMSO. Increasing concentrations are incubated with a His-tagged CRBN protein and a labeled probe. The signal decrease is used to calculate the IC50 and Ki values.
|
| Cell Assay |
Pomalidomide-5-C12-NH2 hydrochloride is a ligand and is not used in a typical cell-based assay alone. The ligand is first conjugated to a linker and a target-binding ligand to form a complete PROTAC. The resulting PROTAC is then tested in cells for its ability to degrade the target protein (measured by Western blot) and inhibit cell proliferation (measured by MTT).
|
| Animal Protocol |
A standard animal protocol for a PROTAC built using Pomalidomide-5-C12-NH2 hydrochloride would involve mouse xenograft models. Mice are implanted with tumor cells. When tumors reach a certain size, mice are treated intraperitoneally or orally with the PROTAC. Tumor growth is measured, and degradation of the target protein is confirmed by Western blot or IHC of tumor lysates.
|
| ADME/Pharmacokinetics |
Pomalidomide-5-C12-NH2 hydrochloride has a molecular weight of 493.04 and the formula C25H37ClN4O4. The product is a solid that should be stored at -20degC for up to 3 years. In solution, it is stable for 1 year at -80degC. It is a pure, solid intermediate that is stable under recommended conditions. Specific PK data are not available.
|
| Toxicity/Toxicokinetics |
Detailed toxicity data for Pomalidomide-5-C12-NH2 hydrochloride are not available. As a research chemical, standard laboratory safety precautions should be followed. The parent compound, Pomalidomide, has a known safety profile, but this derivative is a research intermediate only. Standard safety protocols for handling research chemicals apply.
|
| Additional Infomation |
Pomalidomide-5-C12-NH2 hydrochloride is a research-grade intermediate and is not approved for clinical use. It is a Pomalidomide-based cereblon (CRBN) ligand used in PROTAC synthesis. Its amine group allows for conjugation to protein-targeting ligands, making it a versatile tool for developing selective protein degraders in oncology, immunology, and neurodegenerative disease research.
|
| Molecular Formula |
C25H37CLN4O4
|
|---|---|
| Molecular Weight |
493.04
|
| Appearance |
Light green to green solid powder
|
| 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, 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)
|
| 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 | 2.0282 mL | 10.1412 mL | 20.2823 mL | |
| 5 mM | 0.4056 mL | 2.0282 mL | 4.0565 mL | |
| 10 mM | 0.2028 mL | 1.0141 mL | 2.0282 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
