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 MmrER5l1d3SxeHnjbZR6KEG|c3H5 NW\qXph1OTBizszN MWGyOEBp NUHiOo9jeG:2ZX70cJkh[XWpbXXueJMh\Gm{ZXP0JIFv\CCrbnTpdoVkfCCPTTDj[YxtKGurbHzpcoch[nliU1HS M2W2clI3OzN6Mkez
J-CD38 NH3XWHREgXSxdH;4bYNqfHliQYPzZZk> NUDIU2xCOTBizszN M13ZUVI1KGh? NVzCUIRWeG:2ZX70cJkh[XWpbXXueJMh\Gm{ZXP0JIFv\CCrbnTpdoVkfCCPTTDj[YxtKGurbHzpcoch[nliU1HS NILDbIkzPjN|OEK3Ny=>
R-CD38 NWfyNYtMS3m2b4TvfIlkcXS7IFHzd4F6 MmLGNVAh|ryP NX;Kd4lSOjRiaB?= M2SyXZBwfGWwdHz5JIF2\22nboTzJIRqemWldDDhcoQhcW6maYLlZ5QhVU1iY3XscEBscWyuaX7nJIJ6KFODUh?= MmKzNlY{Ozh{N{O=
BC-3 M{HuSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXr0NVNYOzlvMUK1NEBvVQ>? MUC1JIQ> NYHJcpBGTE2VT9Mg M3LwXWlEPTB;MUC3JI5ONCCrbnjpZol1eyClZXzsJGlEPTB;MUC3JI5ONCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NYP2VFl7OjZzMUm5N|k>
BCBL-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVOzPU0yOjVyIH7N NXjMUFc4PSCm MUnEUXNQyqB? MV\JR|UxRTd2IH7NMEBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 Mlq4NlYyOTl7M{m=
JSC-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1S4U|M6NTF{NUCgcm0> MVq1JIQ> NFqzXY1FVVORwrC= NHjyR5pKSzVyPUO0JI5ONCCrbnjpZol1eyClZXzsJJZq[WKrbHn0fUBld3OnIHTldIVv\GWwdHz5 NF\2bm0zPjFzOUmzPS=>
VG-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1noZlM6NTF{NUCgcm0> M3\JUVUh\A>? MoTOSG1UV8Li MnT4TWM2OD1zMEGgcm0tKGmwaHnibZR{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= NYK2OnB{OjZzMUm5N|k>
UMPEL-1 MmDOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX:zPU0yOjVyIH7N M{PWSlUh\A>? MoHWSG1UV8Li NGHDN4lKSzVyPUOyJI5ONCCrbnjpZol1eyClZXzsJJZq[WKrbHn0fUBld3OnIHTldIVv\GWwdHz5 M2HaZVI3OTF7OUO5
UMPEL-3 NX7vNY8yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXHdFd6OzlvMUK1NEBvVQ>? MWK1JIQ> NEj0RmhFVVORwrC= MkG4TWM2OD1zMUGgcm0tKGmwaHnibZR{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= MVeyOlEyQTl|OR?=
BC-1 M2[1VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rFSVM6NTF{NUCgcm0> NYP3foJOPSCm NUTDUJVTTE2VT9Mg NV;zfY9TUUN3ME23OFQhdk1uIHnubIljcXS|IHPlcIwhfmmjYnnsbZR6KGSxc3Wg[IVx\W6mZX70cJk> M3\JWVI3OTF7OUO5
BCP-1 M1K5NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG[1d|U{QS1zMkWwJI5O NYC1OIhKPSCm NYT4Z5NWTE2VT9Mg MoLzTWM2OD1|OU[gcm0tKGmwaHnibZR{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= M{X2OlI3OTF7OUO5
APK-1 NX3tdFdbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTm[GVZOzlvMUK1NEBvVQ>? Ml[3OUBl NXzYZodETE2VT9Mg MoXmTWM2OD1{Mk[gcm0tKGmwaHnibZR{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= Mm\JNlYyOTl7M{m=
RPMI8226  NYDT[mU5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HGOVAvODFvNUCg{txO MonKOFghcA>? NVTteWFXTE2VT9Mg M4PQWGlEPTB;ODFOwG0> NUK3W5prOjZyOUe4O|I>
OPM2  NFrvT2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYT5[lJCOC5yMT21NEDPxE1? MnnoOFghcA>? MorSSG1UV8Li M3\2dGlEPTB;MUCg{txO NUjveYlDOjZyOUe4O|I>
RPMI8226  NGXobWFHfW6ldHnvckBCe3OjeR?= NHPTVXEyOCEQvF2= NELLN4o1QCCq NX;F[FZsTE2VT9Mg M3e2[pN1emWwZ4To[Y5{KGO7dH;wcIF{dWmlLX71Z4xm[XJic3j1eJRtcW6pIH;mJI1VV1JiYX7kJJAudVSRUjDwdo91\Wmw MkW5NlYxQTd6N{K=
OPM2  M4\sWmZ2dmO2aX;uJGF{e2G7 NHq0SZAyOCEQvF2= NFnDTZE1QCCq NUPw[2hqTE2VT9Mg NYi4TFdNe3S{ZX7neIhmdnNiY4n0c5Bt[XOvaXOtcpVkdGWjcjDzbJV1fGyrbnegc4YhdVSRUjDhcoQheC2vVF;SJJBzd3SnaX6= MWeyOlA6Pzh5Mh?=
RPMI8226 MoqySpVv[3Srb36gRZN{[Xl? NF3YVIIxNjFvMUCg{txO MWe0JIg> Mnr0SG1UV8Li NX7VV4E1cW6lcnXhd4V{KF[HR1[gcXJPSSCneIDy[ZN{cW:w NYHLS5k1OjVyNUO5PVA>
SH-SY5Y  MmDnRZBweHSxc3nzJGF{e2G7 M4joRlI2yqEQvHevcWw> MlTENeKhcA>? NF;GVm5k[XW|ZYOgd5RifGm|dHnjZYxtgSC|aXfubYZq[2GwdDDy[YR2[3Srb36gbY4h[m:2aDDDVGYuKGGwZDDDVGYsS01vaX7keYNm\CCjcH;weI9{cXQEoB?= MV[yOFk4PTJ5Nh?=
JJN3 MnfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYr2TYdIOC5zLUGwNEDPxE1? MlflO|IhcA>? MWnEUXNQ MXHpcohq[mm2czDj[YxtKGe{b4f0bEB{dGmpaITsfS=> M3;JSFI{OTd6M{e4
XG-1 Ml\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUOwMlEuOTByIN88US=> M3;wRVczKGh? MVzEUXNQ M{T2XIlvcGmkaYTzJINmdGxiZ4Lve5Rp MkT5NlMyPzh|N{i=
CD138+  NYrqT3N7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkf2NE4yNTFyMDFOwG0> NXHMTXZ1PzJiaB?= MoXMSG1UVw>? MlzlbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NFHmNnMzOzF5OEO3PC=>
XG-1 MYjGeY5kfGmxbjDBd5NigQ>? NH3z[WQzNzFyMDFOwG0> NVjETI5POjRiaB?= MVPEUXNQ MVjpcohq[mm2czDDR2w{N02LUD2x{tEhdVKQQTDlfJBz\XO|aX;u NEjFO24zOzF5OEO3PC=>
U266 NU[y[ZVVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3O2WFAvODFvMUCg{txO MlnzOFjjiImq NGrQdGlFVVOR NUK3Wlc4cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? M2\TclIzPTV{MEC4
CRBN60 Mme4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LuflAvODFvMUCg{txO NGPGdoI1QOLCiXi= NHvqVVZFVVOR NXe2cWxCcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MX[yNlU2OjByOB?=
CRNB75 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXqwMlAyNTFyIN88US=> M{WwXVQ56oDLaB?= MXvEUXNQ M173WIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> M2HFclIzPTV{MEC4
MM.1S M3HMWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU[wMlAyNTFyIN88US=> M2PaUlQ56oDLaB?= NGLCSHdFVVOR NV\nNms4e2mpbnnmbYNidnSueTDpcohq[mm2czDwdo9tcW[ncnH0bY9vKGG2IHPvcoNmdnS{YYTpc45{KGG|IHzve{BieyByLkCx{txO NULmeJFuOjF|OEmzNlc>
OPM2 NEjQcndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;YZ|YxNjBzLUGwJO69VQ>? NHXIcVM1QOLCiXi= MlfrSG1UVw>? M1:yZZNq\26rZnnjZY51dHliaX7obYJqfHNicILvcIln\XKjdHnvckBifCClb37j[Y51emG2aX;ud{BieyCub4egZZMhOC5yMd88US=> M3foc|IyOzh7M{K3
MM.1S NVfjWYtoTnWwY4Tpc44hSXO|YYm= M3LpTlExKM7:TR?= NHm1bWw4OiCq M3TCSmROW09? Mn2wd4lodmmoaXPhcpRtgSCmZXPy[YF{\XNidHjlJJBzd3SnaX6gcIV3\Wxib3[gR{9GSlEQsjDpd49nd3Kvc9Mg NGr5[VEzOTN6OUOyOy=>
H929 NYe2S2R{TnWwY4Tpc44hSXO|YYm= NWDwRZQ{OTBizszN MXm3NkBp Ml3USG1UVw>? MYTzbYdvcW[rY3HueIx6KGSnY4LlZZNmeyC2aHWgdJJwfGWrbjDs[ZZmdCCxZjDDM2VDWM7{IHnzc4Zwem2|wrC= NXn3R5c6OjF|OEmzNlc>
OPM2 MofCSpVv[3Srb36gRZN{[Xl? NW\aPIY1OTBizszN NHexemU4OiCq NFLOXllFVVOR MX\zbYdvcW[rY3HueIx6KGSnY4LlZZNmeyC2aHWgdJJwfGWrbjDs[ZZmdCCxZjDDM2VDWM7{IHnzc4Zwem2|wrC= NETab|QzOTN6OUOyOy=>
CT26 NULZSWtCTnWwY4Tpc44hSXO|YYm= MoLaNU8yOCEQvF2= MYWyOEBp MmrKdoVlfWOnczD0bIUhdnWvYnXyd{Bw\iCuaY\lJINwdG:waXXzxsA> NICyZ4gyQTZ|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