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
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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

Choose Selective TNF-alpha Inhibitors

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 MWXDfZRwfG:6aXPpeJkhSXO|YYm= NH7jVm0yOCEQvF2= MWmyOEBp NV3idpJWeG:2ZX70cJkh[XWpbXXueJMh\Gm{ZXP0JIFv\CCrbnTpdoVkfCCPTTDj[YxtKGurbHzpcoch[nliU1HS MonKNlY{Ozh{N{O=
J-CD38 Ml;PR5l1d3SxeHnjbZR6KEG|c3H5 NVvEXXhkOTBizszN MVqyOEBp M1r3SZBwfGWwdHz5JIF2\22nboTzJIRqemWldDDhcoQhcW6maYLlZ5QhVU1iY3XscEBscWyuaX7nJIJ6KFODUh?= NFrITGIzPjN|OEK3Ny=>
R-CD38 NF2wfmNEgXSxdH;4bYNqfHliQYPzZZk> M4rFNVExKM7:TR?= NVS5[YtpOjRiaB?= MlXodI91\W62bImgZZVodWWwdIOg[Ilz\WO2IHHu[EBqdmSrcnXjeEBOVSClZXzsJItqdGyrbnegZpkhW0GU M2PDZ|I3OzN6Mkez
BC-3 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUizPU0yOjVyIH7N NUL5SWhQPSCm NV;3V3VsTE2VT9Mg MXTJR|UxRTFyNzDuUUwhcW6qaXLpeJMh[2WubDDJR|UxRTFyNzDuUUwhfmmjYnnsbZR6KGSxc3Wg[IVx\W6mZX70cJk> MYqyOlEyQTl|OR?=
BCBL-1 NEL4UWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPlN|kuOTJ3MDDuUS=> M3T0UVUh\A>? M4rkWGROW00EoB?= NVG5cJJPUUN3ME23OEBvVSxiaX7obYJqfHNiY3XscEB3cWGkaXzpeJkh\G:|ZTDk[ZBmdmSnboTsfS=> M4XX[lI3OTF7OUO5
JSC-1 NFrSWVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLofJU{QS1zMkWwJI5O M13OSVUh\A>? MlLrSG1UV8Li M3iycWlEPTB;M{Sgcm0tKGmwaHnibZR{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= M2nDc|I3OTF7OUO5
VG-1 NXf6NFFKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDxN|kuOTJ3MDDuUS=> NY\kXY9VPSCm MnjqSG1UV8Li NHHGfGdKSzVyPUGwNUBvVSxiaX7obYJqfHNiY3XscEB3cWGkaXzpeJkh\G:|ZTDk[ZBmdmSnboTsfS=> MluzNlYyOTl7M{m=
UMPEL-1 MoP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7DcoJPOzlvMUK1NEBvVQ>? NIXoXJc2KGR? NIfoe4VFVVORwrC= NXjEcmNlUUN3ME2zNkBvVSxiaX7obYJqfHNiY3XscEB3cWGkaXzpeJkh\G:|ZTDk[ZBmdmSnboTsfS=> NEfQZmszPjFzOUmzPS=>
UMPEL-3 MnzaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGT0e4g{QS1zMkWwJI5O M2fibFUh\A>? NX3CW|hQTE2VT9Mg MUDJR|UxRTFzMTDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NVnuXnJ1OjZzMUm5N|k>
BC-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUGzPU0yOjVyIH7N NHXuOHA2KGR? MkXCSG1UV8Li MYXJR|UxRTd2NDDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MmnCNlYyOTl7M{m=
BCP-1 NVPId3l[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFzEb28{QS1zMkWwJI5O MY[1JIQ> MXXEUXNQyqB? NXiwOFdKUUN3ME2zPVYhdk1uIHnubIljcXS|IHPlcIwhfmmjYnnsbZR6KGSxc3Wg[IVx\W6mZX70cJk> M1TjPVI3OTF7OUO5
APK-1 Mmf1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TVRVM6NTF{NUCgcm0> Mn32OUBl NVXhS4U{TE2VT9Mg NH33OGtKSzVyPUKyOkBvVSxiaX7obYJqfHNiY3XscEB3cWGkaXzpeJkh\G:|ZTDk[ZBmdmSnboTsfS=> MWqyOlEyQTl|OR?=
RPMI8226  NHf3OWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PmN|AvODFvNUCg{txO NYTETFdHPDhiaB?= NUPFeXdOTE2VT9Mg NX\rd2lzUUN3ME24JO69VQ>? MlXFNlYxQTd6N{K=
OPM2  NUf1e5ZbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnXZNE4xOS13MDFOwG0> M3:5TVQ5KGh? NHfsW2NFVVORwrC= NEPlW3BKSzVyPUGwJO69VQ>? MkCyNlYxQTd6N{K=
RPMI8226  NE\BbYlHfW6ldHnvckBCe3OjeR?= M4r6RlExKM7:TR?= MYW0PEBp MV;EUXNQyqB? M3LNZ5N1emWwZ4To[Y5{KGO7dH;wcIF{dWmlLX71Z4xm[XJic3j1eJRtcW6pIH;mJI1VV1JiYX7kJJAudVSRUjDwdo91\Wmw NIrMTmUzPjB7N{i3Ni=>
OPM2  MoXZSpVv[3Srb36gRZN{[Xl? NYmw[WxyOTBizszN M171TlQ5KGh? NWPT[Gl[TE2VT9Mg NX;zPXV3e3S{ZX7neIhmdnNiY4n0c5Bt[XOvaXOtcpVkdGWjcjDzbJV1fGyrbnegc4YhdVSRUjDhcoQheC2vVF;SJJBzd3SnaX6= MW[yOlA6Pzh5Mh?=
RPMI8226 NVnsdnhYTnWwY4Tpc44hSXO|YYm= M1HDPFAvOS1zMDFOwG0> M3r4fFQhcA>? MYnEUXNQyqB? MonxbY5kemWjc3XzJHZGT0ZibWLORUBmgHC{ZYPzbY9v NYnReHRVOjVyNUO5PVA>
SH-SY5Y  NX\FOZh[SXCxcITvd4l{KEG|c3H5 NFP4dnYzPcLizsznM41N NEHJco4yyqCq MUXjZZV{\XNic4TheIl{fGmlYXzsfUB{cWewaX\pZ4FvfCC{ZXT1Z5Rqd25iaX6gZo91cCCFUF[tJIFv\CCFUF[rR20ucW6mdXPl[EBieG:ydH;zbZPDqA>? NIjNUowzPDl5NUK3Oi=>
JJN3 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DnSFAvOS1zMECg{txO M4nuflczKGh? NHL3[HJFVVOR M2Lq[olvcGmkaYTzJINmdGxiZ4Lve5RpKHOuaXfoeIx6 MYqyN|E4QDN5OB?=
XG-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYCwMlEuOTByIN88US=> M2DZblczKGh? M3S1VmROW09? NH\wUVRqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NV;s[o06OjNzN{izO|g>
CD138+  M1\KVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYGwMlEuOTByIN88US=> NXjYRnl[PzJiaB?= Mm\1SG1UVw>? MnOybY5pcWKrdIOgZ4VtdCCpcn;3eIg> MWqyN|E4QDN5OB?=
XG-1 NUnWem8yTnWwY4Tpc44hSXO|YYm= MmXBNk8yODBizszN M1qwVlI1KGh? NXnFR|ZkTE2VTx?= M{nX[IlvcGmkaYTzJGNEVDNxTVnQMVHPuSCvUl7BJIV5eHKnc4Ppc44> MYWyN|E4QDN5OB?=
U266 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17oNVAvODFvMUCg{txO MkXYOFjjiImq MUfEUXNQ NUfUbJR{cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MkjpNlI2PTJyMEi=
CRBN60 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLLNE4xOS1zMDFOwG0> NYfXNW9tPDkkgJno NWrRT|RrTE2VTx?= M{HZdIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NX;XNYY4OjJ3NUKwNFg>
CRNB75 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXSNE4xOS1zMDFOwG0> MmXDOFjjiImq NX:0THhTTE2VTx?= MneybY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> MYWyNlU2OjByOB?=
MM.1S NF:xcYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYGwMlAyNTFyIN88US=> NV\MV|FnPDkkgJno NF24W|VFVVOR MmTTd4lodmmoaXPhcpRtgSCrbnjpZol1eyCycn;sbYZmemG2aX;uJIF1KGOxbnPlcpRz[XSrb37zJIF{KGyxdzDhd{AxNjBzzszN M2DlblIyOzh7M{K3
OPM2 NWLQfGVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV[wMlAyNTFyIN88US=> Mn\KOFjjiImq MVXEUXNQ M1f3[pNq\26rZnnjZY51dHliaX7obYJqfHNicILvcIln\XKjdHnvckBifCClb37j[Y51emG2aX;ud{BieyCub4egZZMhOC5yMd88US=> M2jOTVIyOzh7M{K3
MM.1S MXXGeY5kfGmxbjDBd5NigQ>? Ml;1NVAh|ryP MXS3NkBp MWTEUXNQ M4DWTJNq\26rZnnjZY51dHliZHXjdoVie2W|IITo[UBxem:2ZXnuJIxmfmWuIH;mJGMwTUKSzsKgbZNw\m:{bYRCpC=> M1fuXVIyOzh7M{K3
H929 M{m5U2Z2dmO2aX;uJGF{e2G7 NXnpZ2NGOTBizszN M1nXUVczKGh? MoPLSG1UVw>? Mn\xd4lodmmoaXPhcpRtgSCmZXPy[YF{\XNidHjlJJBzd3SnaX6gcIV3\Wxib3[gR{9GSlEQsjDpd49nd3Kvc9Mg NVvtcpVbOjF|OEmzNlc>
OPM2 MYjGeY5kfGmxbjDBd5NigQ>? Mn3RNVAh|ryP MVW3NkBp M3vFcWROW09? NYHTZXMxe2mpbnnmbYNidnSueTDk[YNz\WG|ZYOgeIhmKHC{b4TlbY4hdGW4ZXygc4YhSy:HQmFOtkBqe2:ob4Ltd:Kh NHjKcpMzOTN6OUOyOy=>
CT26 NYizfFFJTnWwY4Tpc44hSXO|YYm= MkTvNU8yOCEQvF2= Mk[5NlQhcA>? NHnq[2Fz\WS3Y3XzJJRp\SCwdX3i[ZJ{KG:oIHzpeoUh[2:ub37p[ZPDqA>? MkPlNVk3Ozh7N{e=

... 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 54 mg/mL (197.62 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
3mg/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.

Chemical Information

Molecular Weight 273.24
Formula

C13H11N3O4

CAS No. 19171-19-8
Storage powder
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

Tech Support

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.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    Is S1567 in the 1% DMSO+30% polyethylene glycol+1% Tween 80 suitable for oral administration?

  • Answer:

    S1567 in 1% DMSO+30% polyethylene glycol+1% Tween 80 is a suspension. This formulation is for oral gavege.

  • Question 2:

    I would like to know if the pomalidomide is racemic or optically active?

  • Answer:

    Our S1567 Pomalidomide is racemic.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID