Pomalidomide

For research use only.

Catalog No.S1567 Synonyms: CC-4047

48 publications

Pomalidomide Chemical Structure

Molecular Weight(MW): 273.24

Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs. Pomalidomide can be utilized in PROTAC as a ligand for targeting E3 ligase and inhibiting the E3 ligase protein cereblon (CRBN). Pomalidomide promotes apoptosis and cell cycle arrest.

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Selleck's Pomalidomide has been cited by 48 publications

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Choose Selective E3 ligase Ligand Inhibitors

Biological Activity

Description Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs. Pomalidomide can be utilized in PROTAC as a ligand for targeting E3 ligase and inhibiting the E3 ligase protein cereblon (CRBN). Pomalidomide promotes apoptosis and cell cycle arrest.
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 MnfsR5l1d3SxeHnjbZR6KEG|c3H5 MV2xNEDPxE1? M135dFI1KGh? MX;wc5RmdnSueTDheYdu\W62czDkbZJm[3RiYX7kJIlv\Gm{ZXP0JG1OKGOnbHygb4ltdGmwZzDifUBUSVJ? NEHBN|UzPjN|OEK3Ny=>
J-CD38 M{\YUmN6fG:2b4jpZ4l1gSCDc4PhfS=> NW\6c|VoOTBizszN MViyOEBp MUfwc5RmdnSueTDheYdu\W62czDkbZJm[3RiYX7kJIlv\Gm{ZXP0JG1OKGOnbHygb4ltdGmwZzDifUBUSVJ? MWWyOlM{QDJ5Mx?=
R-CD38 Mnv5R5l1d3SxeHnjbZR6KEG|c3H5 NVi3UoliOTBizszN MWiyOEBp NIK5eXRxd3SnboTsfUBifWevZX70d{BlcXKnY4SgZY5lKGmwZHny[YN1KE2PIHPlcIwhc2mubHnu[{BjgSCVQWK= NUXSWo9UOjZ|M{iyO|M>
BC-3 NX65XmZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVOzPU0yOjVyIH7N NV:2V|c3PSCm NYK0N5dUTE2VT9Mg MmD6TWM2OD1zMEegcm0tKGmwaHnibZR{KGOnbHygTWM2OD1zMEegcm0tKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MVGyOlEyQTl|OR?=
BCBL-1 MonOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXWzPU0yOjVyIH7N M{PBVVUh\A>? MoPXSG1UV8Li M4rzcmlEPTB;N{Sgcm0tKGmwaHnibZR{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= MmTHNlYyOTl7M{m=
JSC-1 MnW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPrdY0{QS1zMkWwJI5O NHnENJg2KGR? MVTEUXNQyqB? MYrJR|UxRTN2IH7NMEBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M1;pUVI3OTF7OUO5
VG-1 MknBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY[zPU0yOjVyIH7N MWq1JIQ> NV;Fb3F{TE2VT9Mg M1HmeWlEPTB;MUCxJI5ONCCrbnjpZol1eyClZXzsJJZq[WKrbHn0fUBld3OnIHTldIVv\GWwdHz5 M3PRclI3OTF7OUO5
UMPEL-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGX5[o8{QS1zMkWwJI5O NUjZdGVbPSCm MlraSG1UV8Li NVqzTG9GUUN3ME2zNkBvVSxiaX7obYJqfHNiY3XscEB3cWGkaXzpeJkh\G:|ZTDk[ZBmdmSnboTsfS=> MWGyOlEyQTl|OR?=
UMPEL-3 M3:x[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVWzPU0yOjVyIH7N MUG1JIQ> MmruSG1UV8Li MW\JR|UxRTFzMTDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MnXiNlYyOTl7M{m=
BC-1 NYLXPZlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4ixb|M6NTF{NUCgcm0> MkHEOUBl NWS3dY1jTE2VT9Mg M4DTPWlEPTB;N{S0JI5ONCCrbnjpZol1eyClZXzsJJZq[WKrbHn0fUBld3OnIHTldIVv\GWwdHz5 NWfibGRtOjZzMUm5N|k>
BCP-1 NEjLWIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXOfpA4OzlvMUK1NEBvVQ>? M3XJZVUh\A>? MVTEUXNQyqB? NGTxNJBKSzVyPUO5OkBvVSxiaX7obYJqfHNiY3XscEB3cWGkaXzpeJkh\G:|ZTDk[ZBmdmSnboTsfS=> MXWyOlEyQTl|OR?=
APK-1 Mmf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjkNFN7OzlvMUK1NEBvVQ>? NYm2NYhZPSCm NGTUe|JFVVORwrC= MW\JR|UxRTJ{NjDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NGLRU40zPjFzOUmzPS=>
RPMI8226  MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjNN3kxNjBzLUWwJO69VQ>? NGPqT481QCCq M4nTdGROW00EoB?= NWPKb2tUUUN3ME24JO69VQ>? MUGyOlA6Pzh5Mh?=
OPM2  M{S0WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU[wMlAyNTVyIN88US=> NHLCSYI1QCCq M{HKfmROW00EoB?= NF35emxKSzVyPUGwJO69VQ>? M1nFRVI3ODl5OEey
RPMI8226  NYG0WXc1TnWwY4Tpc44hSXO|YYm= MXGxNEDPxE1? Mlv0OFghcA>? MVrEUXNQyqB? M3vQbpN1emWwZ4To[Y5{KGO7dH;wcIF{dWmlLX71Z4xm[XJic3j1eJRtcW6pIH;mJI1VV1JiYX7kJJAudVSRUjDwdo91\Wmw NXnOV21MOjZyOUe4O|I>
OPM2  NF\qW5pHfW6ldHnvckBCe3OjeR?= MljkNVAh|ryP NYLrb3pIPDhiaB?= NVjNb29yTE2VT9Mg M2HBWJN1emWwZ4To[Y5{KGO7dH;wcIF{dWmlLX71Z4xm[XJic3j1eJRtcW6pIH;mJI1VV1JiYX7kJJAudVSRUjDwdo91\Wmw NGnjUZozPjB7N{i3Ni=>
RPMI8226 MVrGeY5kfGmxbjDBd5NigQ>? M3zxPFAvOS1zMDFOwG0> MnfROEBp M3;NW2ROW00EoB?= MWjpcoNz\WG|ZYOgWmVITiCvUl7BJIV5eHKnc4Ppc44> NUH2WG9bOjVyNUO5PVA>
SH-SY5Y  M{LnN2Fxd3C2b4Ppd{BCe3OjeR?= MVmyOeKh|rypL33M MWGxxsBp MULjZZV{\XNic4TheIl{fGmlYXzsfUB{cWewaX\pZ4FvfCC{ZXT1Z5Rqd25iaX6gZo91cCCFUF[tJIFv\CCFUF[rR20ucW6mdXPl[EBieG:ydH;zbZPDqA>? MknGNlQ6PzV{N{[=
JJN3 NIq0PWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVSwUJdzOC5zLUGwNEDPxE1? NF;uNYQ4OiCq NVPhV4hRTE2VTx?= MXTpcohq[mm2czDj[YxtKGe{b4f0bEB{dGmpaITsfS=> MXqyN|E4QDN5OB?=
XG-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnSWpUxNjFvMUCwJO69VQ>? Mnq5O|IhcA>? M4fjVWROW09? NH7uSIVqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MmrONlMyPzh|N{i=
CD138+  NIrsXWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYiyZnFyOC5zLUGwNEDPxE1? MnfEO|IhcA>? NW\o[pkyTE2VTx?= NITFPYJqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M3PnVVI{OTd6M{e4
XG-1 NYnZOY1ETnWwY4Tpc44hSXO|YYm= NHnvWnAzNzFyMDFOwG0> NIHQ[Y8zPCCq NULHXGtCTE2VTx?= MVHpcohq[mm2czDDR2w{N02LUD2x{tEhdVKQQTDlfJBz\XO|aX;u Mn7xNlMyPzh|N{i=
U266 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXqwMlAyNTFyIN88US=> MkjzOFjjiImq NF;tTYRFVVOR M3LDR4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> Mn3FNlI2PTJyMEi=
CRBN60 NWS3fmJrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPH[YMxNjBzLUGwJO69VQ>? MonLOFjjiImq MmK0SG1UVw>? M12wVYlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NFi1N|QzOjV3MkCwPC=>
CRNB75 NH;HWIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HjSFAvODFvMUCg{txO MYO0PQKBkWh? M2r1bWROW09? M3zNS4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> Mn31NlI2PTJyMEi=
MM.1S MnLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrxNE4xOS1zMDFOwG0> Mm\qOFjjiImq MmHJSG1UVw>? NUXMc2RKe2mpbnnmbYNidnSueTDpcohq[mm2czDwdo9tcW[ncnH0bY9vKGG2IHPvcoNmdnS{YYTpc45{KGG|IHzve{BieyByLkCx{txO NIGzT4czOTN6OUOyOy=>
OPM2 NVHQdo5CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\Kc49zOC5yMT2xNEDPxE1? NX\wZodnPDkkgJno M{HQR2ROW09? Mmq1d4lodmmoaXPhcpRtgSCrbnjpZol1eyCycn;sbYZmemG2aX;uJIF1KGOxbnPlcpRz[XSrb37zJIF{KGyxdzDhd{AxNjBzzszN NVLDZlM4OjF|OEmzNlc>
MM.1S NWPMSlZLTnWwY4Tpc44hSXO|YYm= Mki0NVAh|ryP MYK3NkBp NYL0RmpzTE2VTx?= NYnu[G1te2mpbnnmbYNidnSueTDk[YNz\WG|ZYOgeIhmKHC{b4TlbY4hdGW4ZXygc4YhSy:HQmFOtkBqe2:ob4Ltd:Kh NV\2PYtYOjF|OEmzNlc>
H929 M2jKXWZ2dmO2aX;uJGF{e2G7 MUixNEDPxE1? NFHNTYE4OiCq M3rGbGROW09? MlLwd4lodmmoaXPhcpRtgSCmZXPy[YF{\XNidHjlJJBzd3SnaX6gcIV3\Wxib3[gR{9GSlEQsjDpd49nd3Kvc9Mg NYrXXoh1OjF|OEmzNlc>
OPM2 NYS3W3NHTnWwY4Tpc44hSXO|YYm= MmDjNVAh|ryP MV[3NkBp MXrEUXNQ M373TpNq\26rZnnjZY51dHliZHXjdoVie2W|IITo[UBxem:2ZXnuJIxmfmWuIH;mJGMwTUKSzsKgbZNw\m:{bYRCpC=> NF2yS|YzOTN6OUOyOy=>
CT26 NV20OHBXTnWwY4Tpc44hSXO|YYm= M{WwZVEwOTBizszN MXSyOEBp NVTBU3Z[emWmdXPld{B1cGViboXtZoVzeyCxZjDsbZZmKGOxbH;ubYV{yqB? MXSxPVY{QDl5Nx?=

... 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
  • 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
Smiles NC1=C2C(=O)N(C3CCC(=O)NC3=O)C(=O)C2=CC=C1

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04305444 Recruiting Drug: DTRM-555 Relapsed Chronic Lymphocytic Leukemia|Refractory Chronic Lymphocytic Leukemia|Diffuse Large B Cell Lymphoma|Follicular Lymphoma|Richter''s Transformation Zhejiang DTRM Biopharma April 24 2020 Phase 2
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
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

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.

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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.

E3 ligase Ligand Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID