| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
C5 Lenalidomide targets TNF-α production. As a thalidomide analog, the compound modulates the immune system by inhibiting the production of pro-inflammatory cytokines such as TNF-α. The compound is a potent inhibitor of TNF-α production with an IC50 of 100 μM in LPS stimulated human PBMC and 480 nM in whole blood. It can be used in PROTAC studies as a lenalidomide analogue.
|
|---|---|
| ln Vitro |
In cell-free biochemical systems, C5 Lenalidomide inhibits TNF-α production. The compound's activity is typically measured in cell-based assays rather than cell-free systems. As a thalidomide analog, it may interact with the cereblon (CRBN) E3 ubiquitin ligase complex, leading to the degradation of specific target proteins. This mechanism is relevant for its use in PROTAC studies.
|
| ln Vivo |
In cell-based assays, C5 Lenalidomide inhibits TNF-α production with an IC50 of 100 μM in LPS stimulated human PBMC and 480 nM in whole blood. The compound's effects on TNF-α production are assessed in immune cells such as PBMCs. As a thalidomide analog, it may also have immunomodulatory effects and anti-proliferative activity. The compound can be used in PROTAC studies as a lenalidomide analogue.
|
| Enzyme Assay |
The cell-free assay for C5 Lenalidomide typically involves measuring its binding to target proteins such as cereblon (CRBN). This can be assessed using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC). The compound's ability to induce protein degradation in cell-free systems can be evaluated using ubiquitination assays. However, its TNF-α inhibitory activity is primarily measured in cell-based assays.
|
| Cell Assay |
Cell-based assays for C5 Lenalidomide involve culturing human PBMCs and treating them with the compound at concentrations ranging from 0.1 to 1000 μM. Cells are stimulated with LPS to induce TNF-α production. TNF-α levels in the supernatant are measured by ELISA. The IC50 of 100 μM in LPS stimulated human PBMC and 480 nM in whole blood is determined from dose-response curves.
|
| Animal Protocol |
There is no established animal experimental protocol for C5 Lenalidomide specifically. As a lenalidomide analogue, the compound could potentially be evaluated in animal models for its immunomodulatory and anti-tumor effects. Typical studies for lenalidomide analogues involve administration to mice via oral or intraperitoneal routes. Pharmacodynamic endpoints include assessment of TNF-α inhibition, immunomodulation, and anti-tumor efficacy.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of C5 Lenalidomide have not been extensively reported. As a small molecule with a molecular weight of 259.26 g/mol, the compound would be expected to have reasonable oral bioavailability and tissue penetration. The compound is a lenalidomide analogue and may have similar pharmacokinetic properties to lenalidomide. Further pharmacokinetic studies would be required to determine plasma half-life, clearance, and metabolic pathways.
|
| Toxicity/Toxicokinetics |
C5 Lenalidomide is intended for research use only and lacks established toxicity profiles for therapeutic applications. Standard laboratory safety precautions should be observed when handling this chemical reagent. As a thalidomide analog, the compound may have teratogenic effects and should be handled with extreme care. Standard toxicity studies in rodents would be required to determine the safety profile.
|
| References | |
| Additional Infomation |
C5 Lenalidomide is a research-grade compound supplied for immunology and PROTAC studies. It is not an approved pharmaceutical and has no clinical trial history. The compound is a lenalidomide analogue that can be used in PROTAC studies. It is a potent inhibitor of TNF-α production. This product is intended for research use only and is not for human therapeutic applications.
|
| Molecular Formula |
C13H13N3O3
|
|---|---|
| Molecular Weight |
259.26
|
| Exact Mass |
259.095
|
| CAS # |
191732-70-4
|
| PubChem CID |
9816615
|
| Appearance |
Off-white to gray solid powder
|
| Density |
1.5±0.1 g/cm3
|
| Boiling Point |
634.5±55.0 °C at 760 mmHg
|
| Flash Point |
337.5±31.5 °C
|
| Vapour Pressure |
0.0±1.9 mmHg at 25°C
|
| Index of Refraction |
1.672
|
| LogP |
-1.39
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
19
|
| Complexity |
437
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
WLUIQUZGNPAKRL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H13N3O3/c14-8-1-2-9-7(5-8)6-16(13(9)19)10-3-4-11(17)15-12(10)18/h1-2,5,10H,3-4,6,14H2,(H,15,17,18)
|
| Chemical Name |
3-(6-amino-3-oxo-1H-isoindol-2-yl)piperidine-2,6-dione
|
| 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 | 3.8571 mL | 19.2857 mL | 38.5713 mL | |
| 5 mM | 0.7714 mL | 3.8571 mL | 7.7143 mL | |
| 10 mM | 0.3857 mL | 1.9286 mL | 3.8571 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
