For research use only.
Catalog No.S1567 Synonyms: CC-4047
Molecular Weight(MW): 273.24
Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs. Pomalidomide can be utilized in PROTAC as a ligand for targeting E3 ligase and inhibiting the E3 ligase protein cereblon (CRBN). Pomalidomide promotes apoptosis and cell cycle arrest.
Selleck's Pomalidomide has been cited by 48 publications
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|Description||Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs. Pomalidomide can be utilized in PROTAC as a ligand for targeting E3 ligase and inhibiting the E3 ligase protein cereblon (CRBN). Pomalidomide promotes apoptosis and cell cycle arrest.|
|Features||A derivative of thalidomide and up to 10,000 times more potent than thalidomide.|
Pomalidomide inhibits lipopolysaccharide (LPS) stimulated TNF-alpha release in human PBMC and in human whole blood with IC50 values of 13 nM and 25 nM, respectively.  Pomalidomide inhibits the growth of T regulatory cells which is stimulated by IL-2 with an IC50 of ~1 μM.  Treatment with Pomalidomide (6.4 nM-10 μM) increases the production of IL-2 in human peripheral blood T cells, and is slightly more potent in the CD4+ subset than in the CD8+ subset. Pomalidomide is significantly more potent than CC-5013 at elevating IL-2, IL-5, and IL-10 levels, but only slightly more potent than CC-5013 at elevating IFN-γ levels. Pomalidomide enhances SEE and Raji cells induced AP-1 transcriptional activity in Jurkat cells in a dose-dependent manner, with a maximal enhancement of 4-fold at 1 μM.  Exposure of Raji cells to various concentrations of Pomalidomide (2.5-40 μg/mL) for 48 hours leads to a significant decrease in cell proliferation and DNA synthesis. There is a reduction of ~40% compared to vehicle-treated controls. 
|In vivo||Pomalidomide enhances the antitumor effect of rituximab against B-cell lymphomas in severe combined immunodeficient mice. Administration of Pomalidomide in combination with rituximab, gives the mice a median survival period of 74 days compared with 58 days of CC5013/rituximab treatment and 45 days of rituximab nonotherapy. The synergistic effect of Pomalidomide and rituximab can be completely abrogated by depletion of NK cells, supporting the proposal that NK cell expansion is one mechanism by which Pomalidomide may augment rituximab antitumor activity. |
Inhibition of TNF-α synthesis:TNF-α inhibitory activity is measured in lipopolysacharide (LPS) stimulated PBMC. Pomalidomide is added to human PBMCs 1 hour prior to the addition of LPS (1 μg/mL) and incubation continued for an additional 18-20 hours. Supernatants are then harvested, and the concentration of TNF-α in the supernatants is determined by ELISA. The concentration of Pomalidomide that inhibits TNF- production by 50% (IC50) is calculated by nonlinear regression analysis. The human whole blood TNF- inhibition assay is run in a similar fashion to the PBMC assay except that heparinized fresh human whole blood is plated directly into microtiter plates.
-  Muller GW, et al. Bioorg Med Chem Lett, 1999, 9(11), 1625-1630.
-  Galustian C, et al. Cancer Immunol Immunother, 2009, 58(7), 1033-1045.
-  Schafer PH, et al. J Pharmacol Exp Ther, 2003, 305(3), 1222-1232.
|In vitro||DMSO||54 mg/mL (197.62 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04305444||Recruiting||Drug: DTRM-555||Relapsed Chronic Lymphocytic Leukemia|Refractory Chronic Lymphocytic Leukemia|Diffuse Large B Cell Lymphoma|Follicular Lymphoma|Richter''s Transformation||Zhejiang DTRM Biopharma||April 24 2020||Phase 2|
|NCT03798314||Recruiting||Biological: Nivolumab|Drug: Pomalidomide||Recurrent Nervous System Lymphoma|Recurrent Primary Vitreoretinal DLBCL|Refractory Nervous System Lymphoma|Refractory Primary Vitreoretinal DLBCL||Mayo Clinic|National Cancer Institute (NCI)||January 30 2019||Phase 1|
|NCT03683277||Not yet recruiting||Drug: Ixazomib/Pomalidomide/Dexamethasone||Multiple Myeloma|Relapsed and Refractory Multiple Myeloma|Genetic Condition||Intergroupe Francophone du Myelome|AXONAL|Nantes University Hospital|University Hospital Grenoble|EURAXI||October 1 2018||Phase 2|
|NCT03113942||Active not recruiting||Drug: Pomalidomide 2 MG Oral Capsule [Pomalyst]||High Grade Squamous Intra-epithelial Lesion (HSIL)||Kirby Institute||June 14 2017||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
Is S1567 in the 1% DMSO+30% polyethylene glycol+1% Tween 80 suitable for oral administration?
S1567 in 1% DMSO+30% polyethylene glycol+1% Tween 80 is a suspension. This formulation is for oral gavege.
I would like to know if the pomalidomide is racemic or optically active?
Our S1567 Pomalidomide is racemic.