Pomalidomide

Catalog No.S1567 Synonyms: CC-4047

Pomalidomide Chemical Structure

Molecular Weight(MW): 273.24

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

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In DMSO USD 91 In stock
USD 70 In stock
USD 120 In stock
USD 370 In stock

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2 Customer Reviews

  • MM.1S cells were cultured with Len (lenalidomide) or Pom (pomalidomide) for 48 h.

    Blood Cancer Journal, 2015, 5: e312. Pomalidomide purchased from Selleck.

    OPM2 cells stably expressing either NT or CRBN shRNA were seeded and incubated with pomalidomide at the indicated concentration, followed by MTT assay at day 3 after adding drugs. Each experimental condition was performed in triplicate and repeated at least once.

     

     

    Blood 2011 118, 4771-4779. Pomalidomide purchased from Selleck.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs.
Features A derivative of thalidomide and up to 10,000 times more potent than thalidomide.
Targets
TNF-α [1]
(PBMCs)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MOLP-8 Mmf1R5l1d3SxeHnjbZR6KEG|c3H5 MV[xNEDPxE1? Ml3JNlQhcA>? NUfPdVRveG:2ZX70cJkh[XWpbXXueJMh\Gm{ZXP0JIFv\CCrbnTpdoVkfCCPTTDj[YxtKGurbHzpcoch[nliU1HS MnG1NlY{Ozh{N{O=
J-CD38 MoOzR5l1d3SxeHnjbZR6KEG|c3H5 MmL4NVAh|ryP Ml3KNlQhcA>? MXzwc5RmdnSueTDheYdu\W62czDkbZJm[3RiYX7kJIlv\Gm{ZXP0JG1OKGOnbHygb4ltdGmwZzDifUBUSVJ? MYKyOlM{QDJ5Mx?=
R-CD38 MYTDfZRwfG:6aXPpeJkhSXO|YYm= M{TINFExKM7:TR?= NYfyXmZnOjRiaB?= MkDwdI91\W62bImgZZVodWWwdIOg[Ilz\WO2IHHu[EBqdmSrcnXjeEBOVSClZXzsJItqdGyrbnegZpkhW0GU NHjLTIczPjN|OEK3Ny=>
BC-3 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX:zPU0yOjVyIH7N NGmxTmQ2KGR? NVS5b4tiTE2VT9Mg MYnJR|UxRTFyNzDuUUwhcW6qaXLpeJMh[2WubDDJR|UxRTFyNzDuUUwhfmmjYnnsbZR6KGSxc3Wg[IVx\W6mZX70cJk> MnPuNlYyOTl7M{m=
BCBL-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfvN|kuOTJ3MDDuUS=> MVm1JIQ> M3ThZmROW00EoB?= MVLJR|UxRTd2IH7NMEBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MlLXNlYyOTl7M{m=
JSC-1 MnjRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGP2WGg{QS1zMkWwJI5O M17FRVUh\A>? MnzGSG1UV8Li MVfJR|UxRTN2IH7NMEBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NFTmNlYzPjFzOUmzPS=>
VG-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPqW2JDOzlvMUK1NEBvVQ>? M3PUV|Uh\A>? NF;IbVdFVVORwrC= MnTETWM2OD1zMEGgcm0tKGmwaHnibZR{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= NIiye4ozPjFzOUmzPS=>
UMPEL-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTuSJB1OzlvMUK1NEBvVQ>? NX:0PGszPSCm NFezS4ZFVVORwrC= NVra[mVxUUN3ME2zNkBvVSxiaX7obYJqfHNiY3XscEB3cWGkaXzpeJkh\G:|ZTDk[ZBmdmSnboTsfS=> NIrEUlgzPjFzOUmzPS=>
UMPEL-3 NXS1Z2ZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFqxRYI{QS1zMkWwJI5O NFXzXG02KGR? NYW2NIs2TE2VT9Mg M3PYdGlEPTB;MUGxJI5ONCCrbnjpZol1eyClZXzsJJZq[WKrbHn0fUBld3OnIHTldIVv\GWwdHz5 NIPBSo4zPjFzOUmzPS=>
BC-1 Mo\IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUizPU0yOjVyIH7N NHKzSXQ2KGR? NVPmflN[TE2VT9Mg MWHJR|UxRTd2NDDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MWOyOlEyQTl|OR?=
BCP-1 NG[0WmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPwXGo{QS1zMkWwJI5O NXzZe2psPSCm MlToSG1UV8Li NHrVO5dKSzVyPUO5OkBvVSxiaX7obYJqfHNiY3XscEB3cWGkaXzpeJkh\G:|ZTDk[ZBmdmSnboTsfS=> NV3URZduOjZzMUm5N|k>
APK-1 M{\NeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfzem1mOzlvMUK1NEBvVQ>? M{jNcVUh\A>? NYDOblhHTE2VT9Mg MkO5TWM2OD1{Mk[gcm0tKGmwaHnibZR{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= NYXzfY9SOjZzMUm5N|k>
RPMI8226  M3\De2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlK5NE4xOS13MDFOwG0> NGTQbYs1QCCq M4LY[mROW00EoB?= NHS1SnZKSzVyPUig{txO NHvte3AzPjB7N{i3Ni=>
OPM2  MmDyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\PTVAvODFvNUCg{txO NYLrTolbPDhiaB?= MoLySG1UV8Li MUfJR|UxRTFyIN88US=> NF;1VpkzPjB7N{i3Ni=>
RPMI8226  M3fTR2Z2dmO2aX;uJGF{e2G7 M1j6VVExKM7:TR?= MkjqOFghcA>? MX3EUXNQyqB? MWTzeJJmdme2aHXud{BkgXSxcHzhd41q[y2wdXPs[YFzKHOqdYT0cIlv\yCxZjDtWG9TKGGwZDDwMY1VV1JicILveIVqdg>? NVvPenhYOjZyOUe4O|I>
OPM2  NFvYOFdHfW6ldHnvckBCe3OjeR?= NH;kbmIyOCEQvF2= NI\DOXE1QCCq MYrEUXNQyqB? MYPzeJJmdme2aHXud{BkgXSxcHzhd41q[y2wdXPs[YFzKHOqdYT0cIlv\yCxZjDtWG9TKGGwZDDwMY1VV1JicILveIVqdg>? MX6yOlA6Pzh5Mh?=
RPMI8226 NX\zNZVsTnWwY4Tpc44hSXO|YYm= M2Di[|AvOS1zMDFOwG0> M1flVFQhcA>? NXXQcmdjTE2VT9Mg M2rOVYlv[3KnYYPld{BXTUeIIH3SUmEh\XiycnXzd4lwdg>? MVWyOVA2Ozl7MB?=
SH-SY5Y  NWDwO4k1SXCxcITvd4l{KEG|c3H5 M13TXlI2yqEQvHevcWw> MlrMNeKhcA>? NHfDW3hk[XW|ZYOgd5RifGm|dHnjZYxtgSC|aXfubYZq[2GwdDDy[YR2[3Srb36gbY4h[m:2aDDDVGYuKGGwZDDDVGYsS01vaX7keYNm\CCjcH;weI9{cXQEoB?= MlywNlQ6PzV{N{[=
JJN3 NEfCcmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTEWFdDOC5zLUGwNEDPxE1? MYK3NkBp MXrEUXNQ Mn3ZbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2yrZ3j0cJk> NYjtUGlNOjNzN{izO|g>
XG-1 NHLLeWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX2wMlEuOTByIN88US=> NVjtNJg5PzJiaB?= M3\PbWROW09? MUPpcohq[mm2czDj[YxtKGe{b4f0bC=> Mmm1NlMyPzh|N{i=
CD138+  NGjKfpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUGwMlEuOTByIN88US=> NYf4Z3lJPzJiaB?= M1r0d2ROW09? NXLS[nJJcW6qaXLpeJMh[2WubDDndo94fGh? MVmyN|E4QDN5OB?=
XG-1 MkCwSpVv[3Srb36gRZN{[Xl? MUSyM|ExOCEQvF2= MUiyOEBp NYT6NldbTE2VTx?= Mor6bY5pcWKrdIOgR2NNOy:PSWCtNe6yKG2UTlGg[ZhxemW|c3nvci=> NVe2[XF2OjNzN{izO|g>
U266 NX:wU4JKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVuwMlAyNTFyIN88US=> M3fEOVQ56oDLaB?= MUjEUXNQ NEfuWmhqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NYC0XIk2OjJ3NUKwNFg>
CRBN60 M37kW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3SNE4xOS1zMDFOwG0> MUC0PQKBkWh? MmfTSG1UVw>? M2LoPIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MVSyNlU2OjByOB?=
CRNB75 NH7qPZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkP1NE4xOS1zMDFOwG0> NY\hfWJkPDkkgJno NIPOeZpFVVOR NFzFfZJqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NVnXV5pEOjJ3NUKwNFg>
MM.1S NIHKSpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTaOoVMOC5yMT2xNEDPxE1? MXu0PQKBkWh? NFfaW4xFVVOR M4LobJNq\26rZnnjZY51dHliaX7obYJqfHNicILvcIln\XKjdHnvckBifCClb37j[Y51emG2aX;ud{BieyCub4egZZMhOC5yMd88US=> MYGyNVM5QTN{Nx?=
OPM2 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TnXFAvODFvMUCg{txO M{LoOlQ56oDLaB?= Ml;VSG1UVw>? M37xb5Nq\26rZnnjZY51dHliaX7obYJqfHNicILvcIln\XKjdHnvckBifCClb37j[Y51emG2aX;ud{BieyCub4egZZMhOC5yMd88US=> NFHwO3AzOTN6OUOyOy=>
MM.1S NEnPRoxHfW6ldHnvckBCe3OjeR?= NYLERVFNOTBizszN NGDJepY4OiCq MWrEUXNQ NHrwT45{cWewaX\pZ4FvfGy7IHTlZ5Jm[XOnczD0bIUheHKxdHXpckBt\X[nbDDv[kBEN0WEUN8yJIl{d2[xcn3zxsA> M3GwNVIyOzh7M{K3
H929 Ml\XSpVv[3Srb36gRZN{[Xl? MWexNEDPxE1? NYDYfJlXPzJiaB?= NIPUWo1FVVOR M2PiepNq\26rZnnjZY51dHliZHXjdoVie2W|IITo[UBxem:2ZXnuJIxmfmWuIH;mJGMwTUKSzsKgbZNw\m:{bYRCpC=> Mn:1NlE{QDl|Mke=
OPM2 MlvsSpVv[3Srb36gRZN{[Xl? M1LNdVExKM7:TR?= MUm3NkBp NX;OTGV1TE2VTx?= NEXoVW5{cWewaX\pZ4FvfGy7IHTlZ5Jm[XOnczD0bIUheHKxdHXpckBt\X[nbDDv[kBEN0WEUN8yJIl{d2[xcn3zxsA> NHXYcYozOTN6OUOyOy=>
CT26 NHfnXFZHfW6ldHnvckBCe3OjeR?= NGHzVlEyNzFyIN88US=> M2TYc|I1KGh? NFTQ[Ytz\WS3Y3XzJJRp\SCwdX3i[ZJ{KG:oIHzpeoUh[2:ub37p[ZPDqA>? NF24SIIyQTZ|OEm3Oy=>

... Click to View More Cell Line Experimental Data

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]

Protocol

Kinase Assay:[1]
+ Expand

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 Research:[4]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[4]
+ Expand
  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 55 mg/mL (201.28 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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 Information

Molecular Weight 273.24
Formula

C13H11N3O4

CAS No. 19171-19-8
Storage powder
in solvent
Synonyms CC-4047

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01495598 Recruiting Kaposi Sarcoma|Sarcoma, Kaposi National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) December 9, 2011 Phase 1|Phase 2
NCT02659930 Recruiting Kaposi Sarcoma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) January 4, 2016 Phase 1
NCT01688466 Recruiting Graft vs Host Disease|Graft-Versus-Host Disease National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) August 29, 2012 Phase 2
NCT03030261 Not yet recruiting Multiple Myeloma in Relapse Washington University School of Medicine|Bristol-Myers Squibb|Celgene February 28, 2017 Phase 2
NCT03015922 Not yet recruiting Multiple Myeloma University of Leeds|Myeloma UK|Oncolytics Biotech|Celgene Corporation February 2017 Phase 1
NCT02939183 Recruiting Relapsed or Refractory Multiple Myeloma Amgen January 2017 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID