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.

Size Price Stock Quantity  
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 M1fXUGN6fG:2b4jpZ4l1gSCDc4PhfS=> NUDRT3VuOTBizszN MVeyOEBp MXfwc5RmdnSueTDheYdu\W62czDkbZJm[3RiYX7kJIlv\Gm{ZXP0JG1OKGOnbHygb4ltdGmwZzDifUBUSVJ? MYGyOlM{QDJ5Mx?=
J-CD38 MnW3R5l1d3SxeHnjbZR6KEG|c3H5 NWHTfY1xOTBizszN NHL0[YgzPCCq MXPwc5RmdnSueTDheYdu\W62czDkbZJm[3RiYX7kJIlv\Gm{ZXP0JG1OKGOnbHygb4ltdGmwZzDifUBUSVJ? MkPiNlY{Ozh{N{O=
R-CD38 NYDDb4JTS3m2b4TvfIlkcXS7IFHzd4F6 MXGxNEDPxE1? MmPSNlQhcA>? NF20fYRxd3SnboTsfUBifWevZX70d{BlcXKnY4SgZY5lKGmwZHny[YN1KE2PIHPlcIwhc2mubHnu[{BjgSCVQWK= NFPsdWYzPjN|OEK3Ny=>
BC-3 NV3GOm1vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYezPU0yOjVyIH7N MYW1JIQ> MlizSG1UV8Li MYDJR|UxRTFyNzDuUUwhcW6qaXLpeJMh[2WubDDJR|UxRTFyNzDuUUwhfmmjYnnsbZR6KGSxc3Wg[IVx\W6mZX70cJk> MVGyOlEyQTl|OR?=
BCBL-1 M2XMUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX2zPU0yOjVyIH7N NWnDOm44PSCm M4DuPWROW00EoB?= MlvvTWM2OD15NDDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MnLwNlYyOTl7M{m=
JSC-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjk[nA{QS1zMkWwJI5O NU[2eYVIPSCm MoqySG1UV8Li NFzBWmdKSzVyPUO0JI5ONCCrbnjpZol1eyClZXzsJJZq[WKrbHn0fUBld3OnIHTldIVv\GWwdHz5 NYrVNZNPOjZzMUm5N|k>
VG-1 M2r3UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYezPU0yOjVyIH7N MYC1JIQ> MoHrSG1UV8Li NFL4XG5KSzVyPUGwNUBvVSxiaX7obYJqfHNiY3XscEB3cWGkaXzpeJkh\G:|ZTDk[ZBmdmSnboTsfS=> NGG5O2kzPjFzOUmzPS=>
UMPEL-1 NITpdm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWizPU0yOjVyIH7N M3zZR|Uh\A>? NYTZW3hCTE2VT9Mg NWCxNIRqUUN3ME2zNkBvVSxiaX7obYJqfHNiY3XscEB3cWGkaXzpeJkh\G:|ZTDk[ZBmdmSnboTsfS=> MYWyOlEyQTl|OR?=
UMPEL-3 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fFUlM6NTF{NUCgcm0> MVW1JIQ> M{nteGROW00EoB?= MXHJR|UxRTFzMTDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M4PCOFI3OTF7OUO5
BC-1 NI\xU4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXWzPU0yOjVyIH7N MX[1JIQ> MmjiSG1UV8Li MU\JR|UxRTd2NDDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NHvkcnAzPjFzOUmzPS=>
BCP-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnEN|kuOTJ3MDDuUS=> MUG1JIQ> MX7EUXNQyqB? MkLETWM2OD1|OU[gcm0tKGmwaHnibZR{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= NIrhVFkzPjFzOUmzPS=>
APK-1 NV\Fc41NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvlRYJqOzlvMUK1NEBvVQ>? NFjQVo02KGR? Mn\FSG1UV8Li MlfCTWM2OD1{Mk[gcm0tKGmwaHnibZR{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= MWWyOlEyQTl|OR?=
RPMI8226  NVfVWHJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nCWFAvODFvNUCg{txO MWW0PEBp NFzQTm5FVVORwrC= Mm\GTWM2OD16IN88US=> MWKyOlA6Pzh5Mh?=
OPM2  MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjTe3RGOC5yMT21NEDPxE1? MmDsOFghcA>? MV3EUXNQyqB? NX;1PJJrUUN3ME2xNEDPxE1? NVe3XIpxOjZyOUe4O|I>
RPMI8226  M3qzO2Z2dmO2aX;uJGF{e2G7 NUTOTVBVOTBizszN NFfteJA1QCCq MkPxSG1UV8Li MYLzeJJmdme2aHXud{BkgXSxcHzhd41q[y2wdXPs[YFzKHOqdYT0cIlv\yCxZjDtWG9TKGGwZDDwMY1VV1JicILveIVqdg>? M4jHdVI3ODl5OEey
OPM2  M1;xZmZ2dmO2aX;uJGF{e2G7 NVzKVpRqOTBizszN NHm4VYo1QCCq MVrEUXNQyqB? M2HWRpN1emWwZ4To[Y5{KGO7dH;wcIF{dWmlLX71Z4xm[XJic3j1eJRtcW6pIH;mJI1VV1JiYX7kJJAudVSRUjDwdo91\Wmw Mkm2NlYxQTd6N{K=
RPMI8226 M1TKZ2Z2dmO2aX;uJGF{e2G7 M3\RT|AvOS1zMDFOwG0> MoPsOEBp MUHEUXNQyqB? NHPlfGlqdmO{ZXHz[ZMhXkWJRjDtVm5CKGW6cILld5Nqd25? NGrGPYQzPTB3M{m5NC=>
SH-SY5Y  MUfBdI9xfG:|aYOgRZN{[Xl? MXOyOeKh|rypL33M NHj0fpQyyqCq MV\jZZV{\XNic4TheIl{fGmlYXzsfUB{cWewaX\pZ4FvfCC{ZXT1Z5Rqd25iaX6gZo91cCCFUF[tJIFv\CCFUF[rR20ucW6mdXPl[EBieG:ydH;zbZPDqA>? M135U|I1QTd3Mke2
JJN3 M1zSZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3j5[FAvOS1zMECg{txO MlvNO|IhcA>? M4D6[GROW09? MV7pcohq[mm2czDj[YxtKGe{b4f0bEB{dGmpaITsfS=> MnvpNlMyPzh|N{i=
XG-1 M{fsTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjMUHcxNjFvMUCwJO69VQ>? MoXZO|IhcA>? NYX0e2dVTE2VTx?= NXXZ[oJTcW6qaXLpeJMh[2WubDDndo94fGh? NFLkdY4zOzF5OEO3PC=>
CD138+  MnHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nNU|AvOS1zMECg{txO MYG3NkBp NH:5PXNFVVOR M3jBbIlvcGmkaYTzJINmdGxiZ4Lve5Rp M2fRVFI{OTd6M{e4
XG-1 NXvHcXhRTnWwY4Tpc44hSXO|YYm= M3GyNFIwOTByIN88US=> M2HwelI1KGh? MXvEUXNQ MYDpcohq[mm2czDDR2w{N02LUD2x{tEhdVKQQTDlfJBz\XO|aX;u NEfH[4IzOzF5OEO3PC=>
U266 MknaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rJd|AvODFvMUCg{txO NFXkfm81QOLCiXi= MoXISG1UVw>? M3LCNIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NXfRWnhZOjJ3NUKwNFg>
CRBN60 NVvhcWlqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXWxNIFEOC5yMT2xNEDPxE1? NUTtRYJ4PDkkgJno MlzwSG1UVw>? M4fSRYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NGrjUVMzOjV3MkCwPC=>
CRNB75 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrUc3QxNjBzLUGwJO69VQ>? NYOzd5hUPDkkgJno MYTEUXNQ MVjpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NULVdIhOOjJ3NUKwNFg>
MM.1S Mkj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUCwMlAyNTFyIN88US=> MX[0PQKBkWh? NXLscG15TE2VTx?= NET3enN{cWewaX\pZ4FvfGy7IHnubIljcXS|IIDyc4xq\mW{YYTpc44h[XRiY3;uZ4VvfHKjdHnvcpMh[XNibH;3JIF{KDBwMEJOwG0> M33ENFIyOzh7M{K3
OPM2 NGC1S|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXSwMlAyNTFyIN88US=> NEKzSVQ1QOLCiXi= MoL2SG1UVw>? NWrPfmNle2mpbnnmbYNidnSueTDpcohq[mm2czDwdo9tcW[ncnH0bY9vKGG2IHPvcoNmdnS{YYTpc45{KGG|IHzve{BieyByLkCx{txO MVGyNVM5QTN{Nx?=
MM.1S Mkm4SpVv[3Srb36gRZN{[Xl? NFzQUXAyOCEQvF2= NX7GRmJNPzJiaB?= NFmxU2ZFVVOR MWnzbYdvcW[rY3HueIx6KGSnY4LlZZNmeyC2aHWgdJJwfGWrbjDs[ZZmdCCxZjDDM2VDWM7{IHnzc4Zwem2|wrC= M1n5TVIyOzh7M{K3
H929 MoDHSpVv[3Srb36gRZN{[Xl? M3jVUFExKM7:TR?= NH;PVIY4OiCq NFvNcWlFVVOR NITwNZJ{cWewaX\pZ4FvfGy7IHTlZ5Jm[XOnczD0bIUheHKxdHXpckBt\X[nbDDv[kBEN0WEUN8yJIl{d2[xcn3zxsA> M{fHTVIyOzh7M{K3
OPM2 MYXGeY5kfGmxbjDBd5NigQ>? MmCzNVAh|ryP MkXhO|IhcA>? MWTEUXNQ NUjMfY9me2mpbnnmbYNidnSueTDk[YNz\WG|ZYOgeIhmKHC{b4TlbY4hdGW4ZXygc4YhSy:HQmFOtkBqe2:ob4Ltd:Kh MlnRNlE{QDl|Mke=
CT26 NFrqNXVHfW6ldHnvckBCe3OjeR?= M37ESlEwOTBizszN MWGyOEBp MYLy[YR2[2W|IITo[UBvfW2kZYLzJI9nKGyrdnWgZ49td26rZYRCpC=> NGfuZZMyQTZ|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
+ 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
+ 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
+ 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
NCT02807454 Recruiting Multiple Myeloma Celgene Corporation July 2016 Phase 1|Phase 2
NCT02718833 Recruiting Multiple Myeloma Massachusetts General Hospital|Celgene|Bristol-Myers Squibb June 2016 Phase 2
NCT02569320 Recruiting Recurrent Plasma Cell Myeloma Yvonne Efebera|Celgene|Ohio State University Comprehensive Cancer Center May 2016 Phase 1
NCT02726581 Recruiting Multiple Myeloma Bristol-Myers Squibb|AbbVie April 2016 Phase 3
NCT02406222 Recruiting Multiple Myeloma University of Leeds|Myeloma UK|Celgene March 2016 Phase 2
NCT02548962 Recruiting Multiple Myeloma Pharmacyclics|Celgene Corporation March 2016 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID