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
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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

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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 NX;JNY97S3m2b4TvfIlkcXS7IFHzd4F6 NGW3cmkyOCEQvF2= NX[1TFU4OjRiaB?= MWjwc5RmdnSueTDheYdu\W62czDkbZJm[3RiYX7kJIlv\Gm{ZXP0JG1OKGOnbHygb4ltdGmwZzDifUBUSVJ? M3T6[FI3OzN6Mkez
J-CD38 MlLrR5l1d3SxeHnjbZR6KEG|c3H5 NF7MXIcyOCEQvF2= NEnieGwzPCCq MUTwc5RmdnSueTDheYdu\W62czDkbZJm[3RiYX7kJIlv\Gm{ZXP0JG1OKGOnbHygb4ltdGmwZzDifUBUSVJ? MVGyOlM{QDJ5Mx?=
R-CD38 MorRR5l1d3SxeHnjbZR6KEG|c3H5 NGnLeZEyOCEQvF2= Ml\nNlQhcA>? M3XoUpBwfGWwdHz5JIF2\22nboTzJIRqemWldDDhcoQhcW6maYLlZ5QhVU1iY3XscEBscWyuaX7nJIJ6KFODUh?= NWrxfJFwOjZ|M{iyO|M>
BC-3 Ml\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfLN|kuOTJ3MDDuUS=> MV61JIQ> MYjEUXNQyqB? NIn5SmFKSzVyPUGwO{BvVSxiaX7obYJqfHNiY3XscEBKSzVyPUGwO{BvVSxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M4L1XFI3OTF7OUO5
BCBL-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV:zPU0yOjVyIH7N MoftOUBl MV7EUXNQyqB? MnjqTWM2OD15NDDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M1jCPVI3OTF7OUO5
JSC-1 M4fFV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrXN|kuOTJ3MDDuUS=> Mn3WOUBl MWTEUXNQyqB? MlW0TWM2OD1|NDDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M1fXNFI3OTF7OUO5
VG-1 M{X0NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfpTow{QS1zMkWwJI5O M4HHPFUh\A>? NYPoeWtETE2VT9Mg MVzJR|UxRTFyMTDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MY[yOlEyQTl|OR?=
UMPEL-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLwV2g{QS1zMkWwJI5O NUXKdphwPSCm NIrUbm1FVVORwrC= MUDJR|UxRTN{IH7NMEBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M2f1bVI3OTF7OUO5
UMPEL-3 NGXhTnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofmN|kuOTJ3MDDuUS=> M{iyeFUh\A>? NFzs[Y5FVVORwrC= M4rufWlEPTB;MUGxJI5ONCCrbnjpZol1eyClZXzsJJZq[WKrbHn0fUBld3OnIHTldIVv\GWwdHz5 Mom0NlYyOTl7M{m=
BC-1 NVHRW4x{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TaVFM6NTF{NUCgcm0> NUjuUI93PSCm NWW0dYN{TE2VT9Mg NXTuNVU1UUN3ME23OFQhdk1uIHnubIljcXS|IHPlcIwhfmmjYnnsbZR6KGSxc3Wg[IVx\W6mZX70cJk> MYWyOlEyQTl|OR?=
BCP-1 NG\zRlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnkOFByOzlvMUK1NEBvVQ>? M3f4dlUh\A>? M4PKVWROW00EoB?= M3nPO2lEPTB;M{m2JI5ONCCrbnjpZol1eyClZXzsJJZq[WKrbHn0fUBld3OnIHTldIVv\GWwdHz5 MX6yOlEyQTl|OR?=
APK-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX2zPU0yOjVyIH7N NFXzW3E2KGR? MU\EUXNQyqB? MU\JR|UxRTJ{NjDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NX7DflNNOjZzMUm5N|k>
RPMI8226  M17rPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVywMlAyNTVyIN88US=> Mm\KOFghcA>? M4PORWROW00EoB?= NVzZTIxnUUN3ME24JO69VQ>? NY\kfolmOjZyOUe4O|I>
OPM2  NXHpcVFDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF20UWMxNjBzLUWwJO69VQ>? NVjvd3ZkPDhiaB?= MYfEUXNQyqB? NI\ZbnFKSzVyPUGwJO69VQ>? NHf2VYIzPjB7N{i3Ni=>
RPMI8226  NYjFWXljTnWwY4Tpc44hSXO|YYm= NGKwN|IyOCEQvF2= MUW0PEBp NVvPdmV1TE2VT9Mg NETtR2V{fHKnbnf0bIVveyCleYTvdIxie22rYz3ueYNt\WG{IIPoeZR1dGmwZzDv[kBuXE:UIHHu[EBxNW2WT2KgdJJwfGWrbh?= MVOyOlA6Pzh5Mh?=
OPM2  MVjGeY5kfGmxbjDBd5NigQ>? MVqxNEDPxE1? NILpbno1QCCq M3rUZWROW00EoB?= NIftOFl{fHKnbnf0bIVveyCleYTvdIxie22rYz3ueYNt\WG{IIPoeZR1dGmwZzDv[kBuXE:UIHHu[EBxNW2WT2KgdJJwfGWrbh?= NH63XmQzPjB7N{i3Ni=>
RPMI8226 NVzpZoRETnWwY4Tpc44hSXO|YYm= M4m2R|AvOS1zMDFOwG0> MoDyOEBp MYHEUXNQyqB? MX;pcoNz\WG|ZYOgWmVITiCvUl7BJIV5eHKnc4Ppc44> NU\sb3hrOjVyNUO5PVA>
SH-SY5Y  Mmm3RZBweHSxc3nzJGF{e2G7 NWHGd2l3OjYEoN88[{9uVA>? MV:xxsBp NEnvU5Jk[XW|ZYOgd5RifGm|dHnjZYxtgSC|aXfubYZq[2GwdDDy[YR2[3Srb36gbY4h[m:2aDDDVGYuKGGwZDDDVGYsS01vaX7keYNm\CCjcH;weI9{cXQEoB?= MoPRNlQ6PzV{N{[=
JJN3 M2fsS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfRNE4yNTFyMDFOwG0> MlrLO|IhcA>? M1nxUmROW09? MXjpcohq[mm2czDj[YxtKGe{b4f0bEB{dGmpaITsfS=> NWXld5hXOjNzN{izO|g>
XG-1 MnPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DzblAvOS1zMECg{txO NUTFZVBuPzJiaB?= MnHGSG1UVw>? MmXHbY5pcWKrdIOgZ4VtdCCpcn;3eIg> Ml7YNlMyPzh|N{i=
CD138+  M3:4dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnWNE4yNTFyMDFOwG0> MXu3NkBp MYfEUXNQ MnrqbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M2nEWlI{OTd6M{e4
XG-1 NH7GZ|FHfW6ldHnvckBCe3OjeR?= M4jhXlIwOTByIN88US=> MVuyOEBp MnPkSG1UVw>? MXzpcohq[mm2czDDR2w{N02LUD2x{tEhdVKQQTDlfJBz\XO|aX;u MV[yN|E4QDN5OB?=
U266 NHzo[3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4G2U|AvODFvMUCg{txO NYXPO5VGPDkkgJno NYntN5ZjTE2VTx?= MYXpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 MUeyNlU2OjByOB?=
CRBN60 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHuxXZMxNjBzLUGwJO69VQ>? MVi0PQKBkWh? NGe3d4JFVVOR MV\pcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 M3fGS|IzPTV{MEC4
CRNB75 M3i2R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVe5e5ZvOC5yMT2xNEDPxE1? M3zSd|Q56oDLaB?= MVnEUXNQ MY\pcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NXfBN2s6OjJ3NUKwNFg>
MM.1S MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU[wMlAyNTFyIN88US=> Ml7kOFjjiImq MonqSG1UVw>? NEX6SGt{cWewaX\pZ4FvfGy7IHnubIljcXS|IIDyc4xq\mW{YYTpc44h[XRiY3;uZ4VvfHKjdHnvcpMh[XNibH;3JIF{KDBwMEJOwG0> NGe3fHYzOTN6OUOyOy=>
OPM2 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7jcZMxNjBzLUGwJO69VQ>? NVfzPJFlPDkkgJno MWDEUXNQ MVfzbYdvcW[rY3HueIx6KGmwaHnibZR{KHC{b3zp[oVz[XSrb36gZZQh[2:wY3XueJJifGmxboOgZZMhdG:5IHHzJFAvODIQvF2= NHW0dJYzOTN6OUOyOy=>
MM.1S MVfGeY5kfGmxbjDBd5NigQ>? NFPRNVcyOCEQvF2= M4DjWlczKGh? M1XDRWROW09? NGDxc2t{cWewaX\pZ4FvfGy7IHTlZ5Jm[XOnczD0bIUheHKxdHXpckBt\X[nbDDv[kBEN0WEUN8yJIl{d2[xcn3zxsA> NX\3RoM2OjF|OEmzNlc>
H929 MWrGeY5kfGmxbjDBd5NigQ>? MmHiNVAh|ryP NGfLWo44OiCq MX\EUXNQ NWnWOFdKe2mpbnnmbYNidnSueTDk[YNz\WG|ZYOgeIhmKHC{b4TlbY4hdGW4ZXygc4YhSy:HQmFOtkBqe2:ob4Ltd:Kh M3rKTlIyOzh7M{K3
OPM2 MmXqSpVv[3Srb36gRZN{[Xl? MY[xNEDPxE1? MmjuO|IhcA>? M1qxTmROW09? NHnzUnJ{cWewaX\pZ4FvfGy7IHTlZ5Jm[XOnczD0bIUheHKxdHXpckBt\X[nbDDv[kBEN0WEUN8yJIl{d2[xcn3zxsA> MVuyNVM5QTN{Nx?=
CT26 Mn\FSpVv[3Srb36gRZN{[Xl? MlHENU8yOCEQvF2= M175W|I1KGh? MnnWdoVlfWOnczD0bIUhdnWvYnXyd{Bw\iCuaY\lJINwdG:waXXzxsA> NX;aUlF2OTl4M{i5O|c>

... 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