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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Cited by 33 Publications

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 NGLZVWJEgXSxdH;4bYNqfHliQYPzZZk> NFP3cWcyOCEQvF2= M4nZTlI1KGh? MXTwc5RmdnSueTDheYdu\W62czDkbZJm[3RiYX7kJIlv\Gm{ZXP0JG1OKGOnbHygb4ltdGmwZzDifUBUSVJ? NVnZcoFkOjZ|M{iyO|M>
J-CD38 NWe3THBES3m2b4TvfIlkcXS7IFHzd4F6 MnHWNVAh|ryP NXLX[3A5OjRiaB?= NVTkUll[eG:2ZX70cJkh[XWpbXXueJMh\Gm{ZXP0JIFv\CCrbnTpdoVkfCCPTTDj[YxtKGurbHzpcoch[nliU1HS M3\u[lI3OzN6Mkez
R-CD38 MXHDfZRwfG:6aXPpeJkhSXO|YYm= MVKxNEDPxE1? MnW5NlQhcA>? MofhdI91\W62bImgZZVodWWwdIOg[Ilz\WO2IHHu[EBqdmSrcnXjeEBOVSClZXzsJItqdGyrbnegZpkhW0GU NVex[FNHOjZ|M{iyO|M>
BC-3 M1r2cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW[zPU0yOjVyIH7N MYe1JIQ> NVrqcmlNTE2VT9Mg NYrncnFHUUN3ME2xNFchdk1uIHnubIljcXS|IHPlcIwhUUN3ME2xNFchdk1uII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M2jOdFI3OTF7OUO5
BCBL-1 MluxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVizPU0yOjVyIH7N NYrabIVkPSCm NWXBfYtCTE2VT9Mg NUjrb41XUUN3ME23OEBvVSxiaX7obYJqfHNiY3XscEB3cWGkaXzpeJkh\G:|ZTDk[ZBmdmSnboTsfS=> NIXl[m4zPjFzOUmzPS=>
JSC-1 NYDVUmFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY[wNm9ROzlvMUK1NEBvVQ>? M1v4bVUh\A>? NW\1c3pqTE2VT9Mg NFrQSIdKSzVyPUO0JI5ONCCrbnjpZol1eyClZXzsJJZq[WKrbHn0fUBld3OnIHTldIVv\GWwdHz5 MWOyOlEyQTl|OR?=
VG-1 NGrpSIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV6zPU0yOjVyIH7N M4T0eFUh\A>? NVLTZodVTE2VT9Mg Mnr6TWM2OD1zMEGgcm0tKGmwaHnibZR{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= MWKyOlEyQTl|OR?=
UMPEL-1 NXryUHE{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;xbWh6OzlvMUK1NEBvVQ>? NEK4ZWY2KGR? NVfi[nR1TE2VT9Mg MlvZTWM2OD1|MjDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NYXnZ2p2OjZzMUm5N|k>
UMPEL-3 NYn5UJo3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XZZlM6NTF{NUCgcm0> MYC1JIQ> NVv2bXppTE2VT9Mg M{\4VGlEPTB;MUGxJI5ONCCrbnjpZol1eyClZXzsJJZq[WKrbHn0fUBld3OnIHTldIVv\GWwdHz5 MYqyOlEyQTl|OR?=
BC-1 NEjTdYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDXWZlmOzlvMUK1NEBvVQ>? NEDDSJc2KGR? MXXEUXNQyqB? M4rLRWlEPTB;N{S0JI5ONCCrbnjpZol1eyClZXzsJJZq[WKrbHn0fUBld3OnIHTldIVv\GWwdHz5 NELCcmMzPjFzOUmzPS=>
BCP-1 NFvOT4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInuU4k{QS1zMkWwJI5O MmfzOUBl MXvEUXNQyqB? NU\NdJNVUUN3ME2zPVYhdk1uIHnubIljcXS|IHPlcIwhfmmjYnnsbZR6KGSxc3Wg[IVx\W6mZX70cJk> M1L2Z|I3OTF7OUO5
APK-1 MoX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjycXo{QS1zMkWwJI5O NVXGRo5XPSCm NX;kSJU3TE2VT9Mg M1T4UGlEPTB;MkK2JI5ONCCrbnjpZol1eyClZXzsJJZq[WKrbHn0fUBld3OnIHTldIVv\GWwdHz5 NEftN4EzPjFzOUmzPS=>
RPMI8226  MmO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTPR|NsOC5yMT21NEDPxE1? NXPwS41FPDhiaB?= NFLnS4RFVVORwrC= M4flU2lEPTB;ODFOwG0> NWnTVWVFOjZyOUe4O|I>
OPM2  MojMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\O[G1mOC5yMT21NEDPxE1? NW[4XXBSPDhiaB?= NV\xflU{TE2VT9Mg M{n4O2lEPTB;MUCg{txO NEjzR2YzPjB7N{i3Ni=>
RPMI8226  NGrKPWxHfW6ldHnvckBCe3OjeR?= NIjjXHQyOCEQvF2= NHHmNXQ1QCCq MnjhSG1UV8Li MWfzeJJmdme2aHXud{BkgXSxcHzhd41q[y2wdXPs[YFzKHOqdYT0cIlv\yCxZjDtWG9TKGGwZDDwMY1VV1JicILveIVqdg>? MXuyOlA6Pzh5Mh?=
OPM2  M4\yV2Z2dmO2aX;uJGF{e2G7 M4LVSlExKM7:TR?= MnHUOFghcA>? NIex[VhFVVORwrC= NFnncpp{fHKnbnf0bIVveyCleYTvdIxie22rYz3ueYNt\WG{IIPoeZR1dGmwZzDv[kBuXE:UIHHu[EBxNW2WT2KgdJJwfGWrbh?= MWmyOlA6Pzh5Mh?=
RPMI8226 MonDSpVv[3Srb36gRZN{[Xl? M1fnWFAvOS1zMDFOwG0> MUO0JIg> MYfEUXNQyqB? NUHnOZVUcW6lcnXhd4V{KF[HR1[gcXJPSSCneIDy[ZN{cW:w NYLjbFl2OjVyNUO5PVA>
SH-SY5Y  M{PlTGFxd3C2b4Ppd{BCe3OjeR?= MVuyOeKh|rypL33M Mn\KNeKhcA>? MUjjZZV{\XNic4TheIl{fGmlYXzsfUB{cWewaX\pZ4FvfCC{ZXT1Z5Rqd25iaX6gZo91cCCFUF[tJIFv\CCFUF[rR20ucW6mdXPl[EBieG:ydH;zbZPDqA>? MkfBNlQ6PzV{N{[=
JJN3 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjMR|gxNjFvMUCwJO69VQ>? NWHhWGJyPzJiaB?= NHTnNmtFVVOR NWTrOFRXcW6qaXLpeJMh[2WubDDndo94fGhic3zp[4h1dHl? NXX0dplzOjNzN{izO|g>
XG-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTu[mRVOC5zLUGwNEDPxE1? MY[3NkBp MWLEUXNQ M2WweolvcGmkaYTzJINmdGxiZ4Lve5Rp NXLwZXdUOjNzN{izO|g>
CD138+  M{DSOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjaNE4yNTFyMDFOwG0> MoToO|IhcA>? NUDZdHFYTE2VTx?= NEDQTVZqdmirYnn0d{Bk\WyuIHfyc5d1cA>? Ml3rNlMyPzh|N{i=
XG-1 Mnf3SpVv[3Srb36gRZN{[Xl? NIn3UYQzNzFyMDFOwG0> NFrTWHkzPCCq MX7EUXNQ NWTnOpBycW6qaXLpeJMhS0OOMz;NTXAuOc7zIH3SUmEh\XiycnXzd4lwdg>? NWXKS21TOjNzN{izO|g>
U266 NFfFc3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjvXVYxNjBzLUGwJO69VQ>? M1m3fVQ56oDLaB?= MVvEUXNQ MXLpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NID3U48zOjV3MkCwPC=>
CRBN60 M4XuU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;QNE4xOS1zMDFOwG0> MojsOFjjiImq M4jaOmROW09? NYriZWpocW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MX6yNlU2OjByOB?=
CRNB75 MnzOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1P1VVAvODFvMUCg{txO M3zuTFQ56oDLaB?= NVW0VFJvTE2VTx?= MXrpcohq[mm2czDj[YxtKGe{b4f0bEBld3OnIHTldIVv\GWwdHz5 NUH6ZndVOjJ3NUKwNFg>
MM.1S MnjIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXlTJAxNjBzLUGwJO69VQ>? NFzGXmw1QOLCiXi= NHfzS|VFVVOR NFvudZJ{cWewaX\pZ4FvfGy7IHnubIljcXS|IIDyc4xq\mW{YYTpc44h[XRiY3;uZ4VvfHKjdHnvcpMh[XNibH;3JIF{KDBwMEJOwG0> NUfVeZZ1OjF|OEmzNlc>
OPM2 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYGwMlAyNTFyIN88US=> MUC0PQKBkWh? MUXEUXNQ MkTKd4lodmmoaXPhcpRtgSCrbnjpZol1eyCycn;sbYZmemG2aX;uJIF1KGOxbnPlcpRz[XSrb37zJIF{KGyxdzDhd{AxNjBzzszN NFnBVZIzOTN6OUOyOy=>
MM.1S MnvaSpVv[3Srb36gRZN{[Xl? NXG0V4FrOTBizszN MVq3NkBp NVPIeGhTTE2VTx?= MnXId4lodmmoaXPhcpRtgSCmZXPy[YF{\XNidHjlJJBzd3SnaX6gcIV3\Wxib3[gR{9GSlEQsjDpd49nd3Kvc9Mg NXf3d49rOjF|OEmzNlc>
H929 NFvqNGFHfW6ldHnvckBCe3OjeR?= MnXlNVAh|ryP MofDO|IhcA>? NYH0dmxETE2VTx?= M2L0[pNq\26rZnnjZY51dHliZHXjdoVie2W|IITo[UBxem:2ZXnuJIxmfmWuIH;mJGMwTUKSzsKgbZNw\m:{bYRCpC=> M{DiTVIyOzh7M{K3
OPM2 MnKySpVv[3Srb36gRZN{[Xl? NYr1bndKOTBizszN MX63NkBp NELZRYRFVVOR MnTEd4lodmmoaXPhcpRtgSCmZXPy[YF{\XNidHjlJJBzd3SnaX6gcIV3\Wxib3[gR{9GSlEQsjDpd49nd3Kvc9Mg Ml\TNlE{QDl|Mke=
CT26 NEDYO3VHfW6ldHnvckBCe3OjeR?= NWfYToJPOS9zMDFOwG0> M3XTWFI1KGh? MmTwdoVlfWOnczD0bIUhdnWvYnXyd{Bw\iCuaY\lJINwdG:waXXzxsA> Mn;ONVk3Ozh7N{e=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
CEBPβ; 

PubMed: 21389327     


MM.1S, H929, OPM2, or primary myeloma cells were cultured with DMSO, pomalidomide, or lenalidomide at the indicated concentrations for 3 days. Representative results from 3 independent experiments are shown. Cells were then lysed, and cell lysates were an䲧疝Ỵ疞㧀疜膉痘 瘿뾠ՂᾰƌՂĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ՂĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ⟸෕䐺痖暼瘿⟸෕ᾰƌ

IKZF1 / IKZF3 / UBE2G1 / CRBN ; 

PubMed: 30234487     


Immunoblot analysis of SKMM2 cells transduced with lentiviral vectors encoding GFP, UBE2G1 and UBE2G1-C90S. Cells were treated with DMSO vehicle control, LEN or POM at the indicated concentrations for 16 hr.

21389327 30234487
Immunofluorescence
IKZF1; 

PubMed: 29496670     


CD34+ cells were treated with DMSO (0.01%), LEN, or POM (1 μM) for 6 hours. The cells were then fixed and stained for IKZF1 (red color), and nuclear counterstaining was performed with DAPI (blue color). The localization of IKZF1 was observed using a Leica䲧疝Ỵ疞㧀疜膉痘 

29496670
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]
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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]
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  • 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]
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  • 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 interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03798314 Recruiting Biological: Nivolumab|Drug: Pomalidomide Recurrent Nervous System Lymphoma|Recurrent Primary Vitreoretinal DLBCL|Refractory Nervous System Lymphoma|Refractory Primary Vitreoretinal DLBCL Mayo Clinic|National Cancer Institute (NCI) January 30 2019 Phase 1
NCT03567616 Suspended Drug: Venetoclax|Drug: Pomalidomide|Drug: Dexamethasone Multiple Myeloma AbbVie|Celgene October 18 2018 Phase 2
NCT03683277 Not yet recruiting Drug: Ixazomib/Pomalidomide/Dexamethasone Multiple Myeloma|Relapsed and Refractory Multiple Myeloma|Genetic Condition Intergroupe Francophone du Myelome|AXONAL|Nantes University Hospital|University Hospital Grenoble|EURAXI October 1 2018 Phase 2
NCT03113942 Active not recruiting Drug: Pomalidomide 2 MG Oral Capsule [Pomalyst] High Grade Squamous Intra-epithelial Lesion (HSIL) Kirby Institute June 14 2017 Phase 2
NCT03015922 Recruiting Drug: Lenalidomide or Pomalidomide|Biological: REOLYSIN Multiple Myeloma University of Leeds|Myeloma UK|Oncolytics Biotech|Celgene Corporation June 5 2017 Phase 1

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