Pomalidomide

Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM.

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Pomalidomide Chemical Structure

Pomalidomide Chemical Structure
Molecular Weight: 273.24

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Quality Control & MSDS

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Product Description

Biological Activity

Description Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM.
Targets TNF-α [1]
IC50 13 nM
In vitro 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. [1] Pomalidomide inhibits the growth of T regulatory cells which is stimulated by IL-2 with an IC50 of ~1 μM. [2] 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. [3] 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. [4]
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. [4]
Features A derivative of thalidomide and up to 10,000 times more potent than thalidomide.

Protocol(Only for Reference)

Kinase Assay: [1]

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.

Cell Assay: [4]

Cell lines Raji, SU-DHL-4 and SU-DHL-10 cell lines
Concentrations Dissolved in DMSO, final concentrations 2.5-40 μg/mL
Incubation Time 24 or 48 hours
Method For assessment of cell apoptosis, Lymphoma cell lines are exposed to Pomalidomide (5 μg/mL) for 24 hours or 48 hours. The cells are stained with FITC-labeled Annexin V and propidium iodine. Cell apoptosis is analyzed by multicolor flow cytometric analysis using a fluorescence-activated cell sorter/FACStar Plus flow cytometer. Cells are scored as apoptotic if they are Annexin V–positive and propidium iodine–negative/positive (early and late apoptosis, respectively). For determination of cell proliferation, the Lymphoma cell lines are exposed to Pomalidomide (2.5, 5, 10, 20, and 40 μg/mL) for 24 hours or 48 hours. 1 μCi per well (96-well plate) of [3H]-thymidine is added and cells are incubated for another 18 hours. Cells are then harvested using the Harvest system into the 96-well glass filters and [3H]-thymidine uptake is measured using an automated scintillation counter.

Animal Study: [4]

Animal Models Disseminated lymphoma-bearing SCID mice
Formulation Dissolved in DMSO to make a 10 mg/mL stock solution and diluted to a final concentration of 1 mg/mL in sterile 0.9% normal saline.
Dosages 0.5 mg/kg
Administration Injection i.p.
Solubility 1% DMSO/30% polyethylene glycol/1% Tween 80, 15 mg/mL
* 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Muller GW, et al. Bioorg Med Chem Lett, 1999, 9(11), 1625-1630.

[2] Galustian C, et al. Cancer Immunol Immunother, 2009, 58(7), 1033-1045.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-10-24)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02228512 Recruiting Large Cell Lymphoma Arising in KSHV-associated Multicentric Castleman Disease|Primary Effusion Lymphoma National Cancer Institute (NCI)|National Institutes of He  ...more National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) August 2014 Phase 1|Phase 2
NCT02189343 Not yet recruiting Multiple Myeloma Acetylon Pharmaceuticals Incorporated August 2014 Phase 1
NCT02158702 Not yet recruiting Multiple Myeloma|Relapse After Use of Lenalidomide and Bortezomib National University Hospital, Singapore|Celgene Corporation August 2014 Phase 2
NCT01889420 Not yet recruiting Multiple Myeloma in Relapse New Mexico Cancer Care Alliance|Novartis Corporation July 2014 Phase 1
NCT02176213 Recruiting Multiple Myeloma in Relapse|Multiple Myeloma, Refractory Ajai Chari|Celgene Corporation|Mount Sinai School of Medi  ...more Ajai Chari|Celgene Corporation|Mount Sinai School of Medicine June 2014 Phase 2

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Chemical Information

Download Pomalidomide SDF
Molecular Weight (MW) 273.24
Formula

C13H11N3O4

CAS No. 19171-19-8
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 55 mg/mL (201 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 1% DMSO/30% polyethylene glycol/1% Tween 80 15 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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.
Chemical Name 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione

Research Area

Customer Reviews (1)


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Rating
Source Blood 2011 118, 4771-4779. Pomalidomide purchased from Selleck
Method MTT assay
Cell Lines OPM2 cells
Concentrations 0-1000 nM
Incubation Time 3 d
Results OPM2 was subsequently tested with other anti-myeloma drugs, showing resistance to lenalidomide and pomalidomide.

Product Citations (6)

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