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

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 M2TD[WN6fG:2b4jpZ4l1gSCDc4PhfS=> M17lVlExKM7:TR?= NEjaWIwzPCCq NYPUdWtFeG:2ZX70cJkh[XWpbXXueJMh\Gm{ZXP0JIFv\CCrbnTpdoVkfCCPTTDj[YxtKGurbHzpcoch[nliU1HS MXyyOlM{QDJ5Mx?=
J-CD38 Mlv0R5l1d3SxeHnjbZR6KEG|c3H5 NVfMPYppOTBizszN MYmyOEBp MUDwc5RmdnSueTDheYdu\W62czDkbZJm[3RiYX7kJIlv\Gm{ZXP0JG1OKGOnbHygb4ltdGmwZzDifUBUSVJ? MonpNlY{Ozh{N{O=
R-CD38 M2L3UWN6fG:2b4jpZ4l1gSCDc4PhfS=> MkLKNVAh|ryP MV2yOEBp NXjHeVZseG:2ZX70cJkh[XWpbXXueJMh\Gm{ZXP0JIFv\CCrbnTpdoVkfCCPTTDj[YxtKGurbHzpcoch[nliU1HS MmrDNlY{Ozh{N{O=
BC-3 M1TCZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUD4bFh7OzlvMUK1NEBvVQ>? M13wcVUh\A>? MlOySG1UV8Li NF\mb4NKSzVyPUGwO{BvVSxiaX7obYJqfHNiY3XscEBKSzVyPUGwO{BvVSxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MlH5NlYyOTl7M{m=
BCBL-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVyzPU0yOjVyIH7N MWO1JIQ> M4jaXWROW00EoB?= M4PQ[mlEPTB;N{Sgcm0tKGmwaHnibZR{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= NILyb2UzPjFzOUmzPS=>
JSC-1 Ml7zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXkN|kuOTJ3MDDuUS=> M1XsWlUh\A>? MYLEUXNQyqB? MVLJR|UxRTN2IH7NMEBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M1ezdFI3OTF7OUO5
VG-1 NYDHRWhOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFu4O40{QS1zMkWwJI5O M3XoXVUh\A>? MYXEUXNQyqB? NIX3em5KSzVyPUGwNUBvVSxiaX7obYJqfHNiY3XscEB3cWGkaXzpeJkh\G:|ZTDk[ZBmdmSnboTsfS=> NH;SVYIzPjFzOUmzPS=>
UMPEL-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjtepJNOzlvMUK1NEBvVQ>? NXzSWmxoPSCm NYTIXXdETE2VT9Mg NXW5RZNYUUN3ME2zNkBvVSxiaX7obYJqfHNiY3XscEB3cWGkaXzpeJkh\G:|ZTDk[ZBmdmSnboTsfS=> NETyR|YzPjFzOUmzPS=>
UMPEL-3 NHvUZmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\IXos{QS1zMkWwJI5O NI\tPYI2KGR? MYPEUXNQyqB? Mn36TWM2OD1zMUGgcm0tKGmwaHnibZR{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= NWHvbVRUOjZzMUm5N|k>
BC-1 M3jZS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWiyT2l[OzlvMUK1NEBvVQ>? NEX1WIE2KGR? NWHjR|hxTE2VT9Mg NVvROJdIUUN3ME23OFQhdk1uIHnubIljcXS|IHPlcIwhfmmjYnnsbZR6KGSxc3Wg[IVx\W6mZX70cJk> Mmn6NlYyOTl7M{m=
BCP-1 MkDzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PS[VM6NTF{NUCgcm0> NEDwRnQ2KGR? Mn36SG1UV8Li MnHwTWM2OD1|OU[gcm0tKGmwaHnibZR{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= NEDib3EzPjFzOUmzPS=>
APK-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWOzPU0yOjVyIH7N MXO1JIQ> M3ywSWROW00EoB?= M17aTGlEPTB;MkK2JI5ONCCrbnjpZol1eyClZXzsJJZq[WKrbHn0fUBld3OnIHTldIVv\GWwdHz5 M{LGUlI3OTF7OUO5
RPMI8226  MljVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWOwMlAyNTVyIN88US=> MkPSOFghcA>? MVzEUXNQyqB? NGn2W4FKSzVyPUig{txO MWeyOlA6Pzh5Mh?=
OPM2  M3rUdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3sc3oxNjBzLUWwJO69VQ>? MmPtOFghcA>? MUfEUXNQyqB? NF7wdHZKSzVyPUGwJO69VQ>? MYqyOlA6Pzh5Mh?=
RPMI8226  MVvGeY5kfGmxbjDBd5NigQ>? M3nKXlExKM7:TR?= M3rsXlQ5KGh? MUDEUXNQyqB? NXPUc2RNe3S{ZX7neIhmdnNiY4n0c5Bt[XOvaXOtcpVkdGWjcjDzbJV1fGyrbnegc4YhdVSRUjDhcoQheC2vVF;SJJBzd3SnaX6= NUnKdI9COjZyOUe4O|I>
OPM2  MWLGeY5kfGmxbjDBd5NigQ>? NXvUS2lpOTBizszN MVq0PEBp NX\YOHU2TE2VT9Mg NHfoe2Z{fHKnbnf0bIVveyCleYTvdIxie22rYz3ueYNt\WG{IIPoeZR1dGmwZzDv[kBuXE:UIHHu[EBxNW2WT2KgdJJwfGWrbh?= NUXUW3Y4OjZyOUe4O|I>
RPMI8226 MmHySpVv[3Srb36gRZN{[Xl? NHToXXkxNjFvMUCg{txO NFvYSYY1KGh? M1jRNGROW00EoB?= NEH4b3lqdmO{ZXHz[ZMhXkWJRjDtVm5CKGW6cILld5Nqd25? NXq0PHRTOjVyNUO5PVA>
SH-SY5Y  M{TQTGFxd3C2b4Ppd{BCe3OjeR?= NWPXd4tIOjYEoN88[{9uVA>? NX3EbndJOcLiaB?= NI\yOVlk[XW|ZYOgd5RifGm|dHnjZYxtgSC|aXfubYZq[2GwdDDy[YR2[3Srb36gbY4h[m:2aDDDVGYuKGGwZDDDVGYsS01vaX7keYNm\CCjcH;weI9{cXQEoB?= NUSzTnYzOjR7N{WyO|Y>
JJN3 MmPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33RcVAvOS1zMECg{txO NXHDd4FRPzJiaB?= MnrUSG1UVw>? Mk\obY5pcWKrdIOgZ4VtdCCpcn;3eIghe2yrZ3j0cJk> NVvxb44{OjNzN{izO|g>
XG-1 NWH3bFBpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfF[2J5OC5zLUGwNEDPxE1? MmDsO|IhcA>? MlvRSG1UVw>? M{\ZdYlvcGmkaYTzJINmdGxiZ4Lve5Rp NGrmT2MzOzF5OEO3PC=>
CD138+  MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\aNE4yNTFyMDFOwG0> MYe3NkBp NVLpcYljTE2VTx?= M3K5[olvcGmkaYTzJINmdGxiZ4Lve5Rp M{PqV|I{OTd6M{e4
XG-1 MlLxSpVv[3Srb36gRZN{[Xl? MXWyM|ExOCEQvF2= MXqyOEBp MoPlSG1UVw>? MV7pcohq[mm2czDDR2w{N02LUD2x{tEhdVKQQTDlfJBz\XO|aX;u MUmyN|E4QDN5OB?=
U266 M1L1b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrxbIl7OC5yMT2xNEDPxE1? NEDvcWc1QOLCiXi= MnPVSG1UVw>? M1zUbIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MUeyNlU2OjByOB?=
CRBN60 NEPXOXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3mcXQxNjBzLUGwJO69VQ>? MkfLOFjjiImq MWrEUXNQ NYroSVc{cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NYnCUmNXOjJ3NUKwNFg>
CRNB75 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TCclAvODFvMUCg{txO MYq0PQKBkWh? NUj0eVhSTE2VTx?= NYC5RpZZcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MoC4NlI2PTJyMEi=
MM.1S NX3neYRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXSTngxNjBzLUGwJO69VQ>? NYT5WWp{PDkkgJno MYDEUXNQ NVXYS2dIe2mpbnnmbYNidnSueTDpcohq[mm2czDwdo9tcW[ncnH0bY9vKGG2IHPvcoNmdnS{YYTpc45{KGG|IHzve{BieyByLkCx{txO M4DuflIyOzh7M{K3
OPM2 MoPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M163TFAvODFvMUCg{txO M2TMeFQ56oDLaB?= MWfEUXNQ NH;me29{cWewaX\pZ4FvfGy7IHnubIljcXS|IIDyc4xq\mW{YYTpc44h[XRiY3;uZ4VvfHKjdHnvcpMh[XNibH;3JIF{KDBwMEJOwG0> MkjKNlE{QDl|Mke=
MM.1S MYPGeY5kfGmxbjDBd5NigQ>? NFfDWoMyOCEQvF2= MlXRO|IhcA>? MoD2SG1UVw>? NFTaOXp{cWewaX\pZ4FvfGy7IHTlZ5Jm[XOnczD0bIUheHKxdHXpckBt\X[nbDDv[kBEN0WEUN8yJIl{d2[xcn3zxsA> NHOxeW8zOTN6OUOyOy=>
H929 NYS1U2FUTnWwY4Tpc44hSXO|YYm= NGHOV3IyOCEQvF2= NHLQW2s4OiCq M{L3W2ROW09? MVHzbYdvcW[rY3HueIx6KGSnY4LlZZNmeyC2aHWgdJJwfGWrbjDs[ZZmdCCxZjDDM2VDWM7{IHnzc4Zwem2|wrC= M1LhZ|IyOzh7M{K3
OPM2 MkO0SpVv[3Srb36gRZN{[Xl? MmT1NVAh|ryP M2LSU|czKGh? MVvEUXNQ Mmjzd4lodmmoaXPhcpRtgSCmZXPy[YF{\XNidHjlJJBzd3SnaX6gcIV3\Wxib3[gR{9GSlEQsjDpd49nd3Kvc9Mg NWnn[IpEOjF|OEmzNlc>
CT26 MnjySpVv[3Srb36gRZN{[Xl? M2fPVlEwOTBizszN MYKyOEBp MnvwdoVlfWOnczD0bIUhdnWvYnXyd{Bw\iCuaY\lJINwdG:waXXzxsA> M4jVb|E6PjN6OUe3

... 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 individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
15 mg/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
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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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID