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 NGj5NZdEgXSxdH;4bYNqfHliQYPzZZk> NUGxZpdqOTBizszN Ml;GNlQhcA>? NFjWXFBxd3SnboTsfUBifWevZX70d{BlcXKnY4SgZY5lKGmwZHny[YN1KE2PIHPlcIwhc2mubHnu[{BjgSCVQWK= MVWyOlM{QDJ5Mx?=
J-CD38 MkKxR5l1d3SxeHnjbZR6KEG|c3H5 M1fjRlExKM7:TR?= NILsS5AzPCCq Ml;6dI91\W62bImgZZVodWWwdIOg[Ilz\WO2IHHu[EBqdmSrcnXjeEBOVSClZXzsJItqdGyrbnegZpkhW0GU MWKyOlM{QDJ5Mx?=
R-CD38 M4HCc2N6fG:2b4jpZ4l1gSCDc4PhfS=> NV6z[2JZOTBizszN NFOxV|czPCCq MUPwc5RmdnSueTDheYdu\W62czDkbZJm[3RiYX7kJIlv\Gm{ZXP0JG1OKGOnbHygb4ltdGmwZzDifUBUSVJ? M4eyNlI3OzN6Mkez
BC-3 NX3lXXA3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEfTPGg{QS1zMkWwJI5O NGLQXWM2KGR? NFjKUXdFVVORwrC= MYTJR|UxRTFyNzDuUUwhcW6qaXLpeJMh[2WubDDJR|UxRTFyNzDuUUwhfmmjYnnsbZR6KGSxc3Wg[IVx\W6mZX70cJk> NWixNHlmOjZzMUm5N|k>
BCBL-1 M{PTZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPDN|kuOTJ3MDDuUS=> M{\UXlUh\A>? MXvEUXNQyqB? NGPSR5JKSzVyPUe0JI5ONCCrbnjpZol1eyClZXzsJJZq[WKrbHn0fUBld3OnIHTldIVv\GWwdHz5 MofMNlYyOTl7M{m=
JSC-1 NXXkZ3RDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVSzPU0yOjVyIH7N MW[1JIQ> MnXKSG1UV8Li NUfofYtiUUN3ME2zOEBvVSxiaX7obYJqfHNiY3XscEB3cWGkaXzpeJkh\G:|ZTDk[ZBmdmSnboTsfS=> M1SybFI3OTF7OUO5
VG-1 NX3zPINnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXGzPU0yOjVyIH7N NUTubZRTPSCm NVju[2VYTE2VT9Mg NGH0SoxKSzVyPUGwNUBvVSxiaX7obYJqfHNiY3XscEB3cWGkaXzpeJkh\G:|ZTDk[ZBmdmSnboTsfS=> M2TJN|I3OTF7OUO5
UMPEL-1 M3fnW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWizPU0yOjVyIH7N Mm[2OUBl NIP5U2NFVVORwrC= MYPJR|UxRTN{IH7NMEBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NEf4cJMzPjFzOUmzPS=>
UMPEL-3 NYjP[YFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXJOIY{QS1zMkWwJI5O NFe1O4Q2KGR? NIHz[ItFVVORwrC= NXf0PGp6UUN3ME2xNVEhdk1uIHnubIljcXS|IHPlcIwhfmmjYnnsbZR6KGSxc3Wg[IVx\W6mZX70cJk> NWHzNYxrOjZzMUm5N|k>
BC-1 MmKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInMcIQ{QS1zMkWwJI5O M1j1Z|Uh\A>? MYPEUXNQyqB? MmXFTWM2OD15NESgcm0tKGmwaHnibZR{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= NHPQUW0zPjFzOUmzPS=>
BCP-1 NX\BdYwzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXGzPU0yOjVyIH7N MnP1OUBl NHHrcldFVVORwrC= NWntR2xUUUN3ME2zPVYhdk1uIHnubIljcXS|IHPlcIwhfmmjYnnsbZR6KGSxc3Wg[IVx\W6mZX70cJk> M1i4NlI3OTF7OUO5
APK-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDGeFI6OzlvMUK1NEBvVQ>? NGfucZI2KGR? M1vOSmROW00EoB?= NFHtbZNKSzVyPUKyOkBvVSxiaX7obYJqfHNiY3XscEB3cWGkaXzpeJkh\G:|ZTDk[ZBmdmSnboTsfS=> M3:4RlI3OTF7OUO5
RPMI8226  NHy2RmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXywMlAyNTVyIN88US=> NIjqZpI1QCCq NYr5WZF5TE2VT9Mg NH\lWW5KSzVyPUig{txO M1;iblI3ODl5OEey
OPM2  NWXUUGFiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHsNE4xOS13MDFOwG0> MWG0PEBp M{WzVWROW00EoB?= NIr5ZldKSzVyPUGwJO69VQ>? NUHnXppbOjZyOUe4O|I>
RPMI8226  MYrGeY5kfGmxbjDBd5NigQ>? MYCxNEDPxE1? MlLvOFghcA>? MlHXSG1UV8Li M2DM[JN1emWwZ4To[Y5{KGO7dH;wcIF{dWmlLX71Z4xm[XJic3j1eJRtcW6pIH;mJI1VV1JiYX7kJJAudVSRUjDwdo91\Wmw MX[yOlA6Pzh5Mh?=
OPM2  M33ab2Z2dmO2aX;uJGF{e2G7 MWWxNEDPxE1? MYW0PEBp MWfEUXNQyqB? M1LkWZN1emWwZ4To[Y5{KGO7dH;wcIF{dWmlLX71Z4xm[XJic3j1eJRtcW6pIH;mJI1VV1JiYX7kJJAudVSRUjDwdo91\Wmw MYmyOlA6Pzh5Mh?=
RPMI8226 NGPOT4JHfW6ldHnvckBCe3OjeR?= NH[y[|IxNjFvMUCg{txO MUS0JIg> NVHrNGx2TE2VT9Mg MoDLbY5kemWjc3XzJHZGT0ZibWLORUBmgHC{ZYPzbY9v MW[yOVA2Ozl7MB?=
SH-SY5Y  M3myOGFxd3C2b4Ppd{BCe3OjeR?= M1vzZVI2yqEQvHevcWw> Mnr3NeKhcA>? NYjqO2Jo[2G3c3XzJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSgdoVlfWO2aX;uJIlvKGKxdHigR3BHNSCjbnSgR3BHM0OPLXnu[JVk\WRiYYDvdJRwe2m|wrC= NETvcYEzPDl5NUK3Oi=>
JJN3 NVjpUnhIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XVflAvOS1zMECg{txO M1TnVVczKGh? MlzUSG1UVw>? NELaZ2VqdmirYnn0d{Bk\WyuIHfyc5d1cCC|bHnnbJRtgQ>? Ml;lNlMyPzh|N{i=
XG-1 NX\COZliT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HDfFAvOS1zMECg{txO MknmO|IhcA>? NFrt[HBFVVOR NGH2SXFqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MmTUNlMyPzh|N{i=
CD138+  NFLBUXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWewMlEuOTByIN88US=> NYjTU2s5PzJiaB?= Mor2SG1UVw>? NUf6c2RLcW6qaXLpeJMh[2WubDDndo94fGh? NWDw[m1sOjNzN{izO|g>
XG-1 M3HJZWZ2dmO2aX;uJGF{e2G7 M{C0R|IwOTByIN88US=> MXWyOEBp M4mwcGROW09? MYLpcohq[mm2czDDR2w{N02LUD2x{tEhdVKQQTDlfJBz\XO|aX;u M{fhfFI{OTd6M{e4
U266 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYqwMlAyNTFyIN88US=> MmH2OFjjiImq NH;j[5JFVVOR NYPYc3J2cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MlWzNlI2PTJyMEi=
CRBN60 M3PpVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVP5S4R7OC5yMT2xNEDPxE1? NIraTm81QOLCiXi= MYPEUXNQ MnfObY5pcWKrdIOgZ4VtdCCpcn;3eIgh\G:|ZTDk[ZBmdmSnboTsfS=> M2G5SVIzPTV{MEC4
CRNB75 NIPoTVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPxNE4xOS1zMDFOwG0> M4H0[FQ56oDLaB?= MoTySG1UVw>? NFy1PY5qdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 NHvZT|IzOjV3MkCwPC=>
MM.1S MmjvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2X2flAvODFvMUCg{txO NWjUPGYxPDkkgJno M4rqSmROW09? NI\lTI5{cWewaX\pZ4FvfGy7IHnubIljcXS|IIDyc4xq\mW{YYTpc44h[XRiY3;uZ4VvfHKjdHnvcpMh[XNibH;3JIF{KDBwMEJOwG0> MkDNNlE{QDl|Mke=
OPM2 NX;4[I5tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFziO20xNjBzLUGwJO69VQ>? NIT2V3U1QOLCiXi= NWjpcFl3TE2VTx?= M1jGUZNq\26rZnnjZY51dHliaX7obYJqfHNicILvcIln\XKjdHnvckBifCClb37j[Y51emG2aX;ud{BieyCub4egZZMhOC5yMd88US=> M2\WeVIyOzh7M{K3
MM.1S MX;GeY5kfGmxbjDBd5NigQ>? NXG3eVRoOTBizszN M1WyOVczKGh? MXHEUXNQ NEfOToF{cWewaX\pZ4FvfGy7IHTlZ5Jm[XOnczD0bIUheHKxdHXpckBt\X[nbDDv[kBEN0WEUN8yJIl{d2[xcn3zxsA> MWWyNVM5QTN{Nx?=
H929 NX3XUXRUTnWwY4Tpc44hSXO|YYm= NIPuXJcyOCEQvF2= MmOyO|IhcA>? NX3OSIVHTE2VTx?= NHTXOJF{cWewaX\pZ4FvfGy7IHTlZ5Jm[XOnczD0bIUheHKxdHXpckBt\X[nbDDv[kBEN0WEUN8yJIl{d2[xcn3zxsA> MkjCNlE{QDl|Mke=
OPM2 MoTVSpVv[3Srb36gRZN{[Xl? MVSxNEDPxE1? NIK3fpM4OiCq MVjEUXNQ NGH6[Wp{cWewaX\pZ4FvfGy7IHTlZ5Jm[XOnczD0bIUheHKxdHXpckBt\X[nbDDv[kBEN0WEUN8yJIl{d2[xcn3zxsA> M{X6dVIyOzh7M{K3
CT26 Mm\uSpVv[3Srb36gRZN{[Xl? NFLoeIMyNzFyIN88US=> M4i3XVI1KGh? NF7Q[mlz\WS3Y3XzJJRp\SCwdX3i[ZJ{KG:oIHzpeoUh[2:ub37p[ZPDqA>? MXKxPVY{QDl5Nx?=

... 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(Data is from Selleck tests instead of citations):
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
in solvent
Synonyms CC-4047

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02569320 Suspended Recurrent Plasma Cell Myeloma Yvonne Efebera|Celgene|Ohio State University Comprehensive Cancer Center May 9 2016 Phase 1
NCT01559129 Completed Scleroderma Systemic|Sclerosis Systemic|Systemic Scleroderma|Systemic Sclerosis Celgene August 9 2012 Phase 2
NCT01722305 Active not recruiting B-Cell Lymphoma Unclassifiable With Features Intermediate Between Diffuse Large B-Cell Lymphoma and Burkitt Lymphoma|Central Nervous System Lymphoma|Intraocular Lymphoma|Primary Diffuse Large B-Cell Lymphoma of the Central Nervous System|Recurrent Adult Diffuse Large Cell Lymphoma|Retinal Lymphoma Mayo Clinic|National Cancer Institute (NCI) April 8 2013 Phase 1
NCT01178281 Active not recruiting Primary Myelofibrosis Celgene September 8 2010 Phase 3
NCT02400242 Active not recruiting Multiple Myeloma Celgene May 7 2015 Phase 1
NCT01734928 Active not recruiting Multiple Myeloma Celgene January 7 2013 Phase 3

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