Pomalidomide

製品コードS1567 別名:CC-4047

Pomalidomide化学構造

分子量(MW):273.24

Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs.

サイズ 価格(税別)  
JPY 15106.00
JPY 11620.00
JPY 19920.00
JPY 61420.00

カスタマーフィードバック(2)

  • 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.

製品安全説明書

TNF-alpha阻害剤の選択性比較

生物活性

製品説明 Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs.
特性 A derivative of thalidomide and up to 10,000 times more potent than thalidomide.
ターゲット
TNF-α [1]
(PBMCs)
13 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MOLP-8 NFf1c5hEgXSxdH;4bYNqfHliQYPzZZk> MlO2NVAh|ryP MXeyOEBp NV3kRZdXeG:2ZX70cJkh[XWpbXXueJMh\Gm{ZXP0JIFv\CCrbnTpdoVkfCCPTTDj[YxtKGurbHzpcoch[nliU1HS MoLuNlY{Ozh{N{O=
J-CD38 MULDfZRwfG:6aXPpeJkhSXO|YYm= M1LtN|ExKM7:TR?= Mm[1NlQhcA>? MmjFdI91\W62bImgZZVodWWwdIOg[Ilz\WO2IHHu[EBqdmSrcnXjeEBOVSClZXzsJItqdGyrbnegZpkhW0GU M2\keFI3OzN6Mkez
R-CD38 M4nSN2N6fG:2b4jpZ4l1gSCDc4PhfS=> M4XzdlExKM7:TR?= Ml;jNlQhcA>? NU\OUoJqeG:2ZX70cJkh[XWpbXXueJMh\Gm{ZXP0JIFv\CCrbnTpdoVkfCCPTTDj[YxtKGurbHzpcoch[nliU1HS MViyOlM{QDJ5Mx?=
BC-3 MorTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7TZW5qOzlvMUK1NEBvVQ>? MV61JIQ> MnrKSG1UV8Li NVLtPGg{UUN3ME2xNFchdk1uIHnubIljcXS|IHPlcIwhUUN3ME2xNFchdk1uII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NV;zN5dXOjZzMUm5N|k>
BCBL-1 NYHYS5V5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHPN|kuOTJ3MDDuUS=> NYHGNY9lPSCm M4\rb2ROW00EoB?= NILNfHFKSzVyPUe0JI5ONCCrbnjpZol1eyClZXzsJJZq[WKrbHn0fUBld3OnIHTldIVv\GWwdHz5 MkTINlYyOTl7M{m=
JSC-1 NWPIOIR1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHCNZQ{QS1zMkWwJI5O NHvMcHI2KGR? M4X5emROW00EoB?= MVfJR|UxRTN2IH7NMEBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 M2L2VFI3OTF7OUO5
VG-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nCNlM6NTF{NUCgcm0> MXW1JIQ> MVPEUXNQyqB? MX\JR|UxRTFyMTDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NEL2N2EzPjFzOUmzPS=>
UMPEL-1 MlXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHNV|M{QS1zMkWwJI5O NWfCcXNUPSCm MlvlSG1UV8Li Mk[yTWM2OD1|MjDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MWGyOlEyQTl|OR?=
UMPEL-3 M3PZVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTmN|kuOTJ3MDDuUS=> MoT5OUBl MUDEUXNQyqB? NX3VU45{UUN3ME2xNVEhdk1uIHnubIljcXS|IHPlcIwhfmmjYnnsbZR6KGSxc3Wg[IVx\W6mZX70cJk> M4XwXlI3OTF7OUO5
BC-1 MnzRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvmN|kuOTJ3MDDuUS=> Mn7vOUBl M{P3bmROW00EoB?= MVPJR|UxRTd2NDDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M3HMNlI3OTF7OUO5
BCP-1 M4TMR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPDN|kuOTJ3MDDuUS=> MoLoOUBl NXLa[JlsTE2VT9Mg Mny4TWM2OD1|OU[gcm0tKGmwaHnibZR{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= M3XmXlI3OTF7OUO5
APK-1 NF3wZllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrtN|kuOTJ3MDDuUS=> MnP0OUBl NFX1NXpFVVORwrC= M3fOcmlEPTB;MkK2JI5ONCCrbnjpZol1eyClZXzsJJZq[WKrbHn0fUBld3OnIHTldIVv\GWwdHz5 NYni[ItyOjZzMUm5N|k>
RPMI8226  NEXleZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LySlAvODFvNUCg{txO MWK0PEBp M2XWPWROW00EoB?= NGmz[WpKSzVyPUig{txO M1:2O|I3ODl5OEey
OPM2  Mnj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFy3OnIxNjBzLUWwJO69VQ>? M2XQT|Q5KGh? MnzrSG1UV8Li MoXZTWM2OD1zMDFOwG0> M2PqNlI3ODl5OEey
RPMI8226  MVTGeY5kfGmxbjDBd5NigQ>? MYWxNEDPxE1? Mkf0OFghcA>? NWmxS2UxTE2VT9Mg MnHRd5Rz\W6pdHjlcpMh[3m2b4DsZZNucWNvboXjcIVieiC|aIX0eIxqdmdib3[gcXRQWiCjbnSgdE1uXE:UIIDyc5RmcW5? M3fiN|I3ODl5OEey
OPM2  NFOwTZNHfW6ldHnvckBCe3OjeR?= M1;6bFExKM7:TR?= M{Xld|Q5KGh? MmC5SG1UV8Li NEnBeGd{fHKnbnf0bIVveyCleYTvdIxie22rYz3ueYNt\WG{IIPoeZR1dGmwZzDv[kBuXE:UIHHu[EBxNW2WT2KgdJJwfGWrbh?= M4PrPFI3ODl5OEey
RPMI8226 M160XmZ2dmO2aX;uJGF{e2G7 MnvuNE4yNTFyIN88US=> NFTPcGo1KGh? MlfmSG1UV8Li M13xZ4lv[3KnYYPld{BXTUeIIH3SUmEh\XiycnXzd4lwdg>? MnHJNlUxPTN7OUC=
SH-SY5Y  MkLIRZBweHSxc3nzJGF{e2G7 NFfQVmQzPcLizsznM41N Mmf0NeKhcA>? NVPBRoQy[2G3c3XzJJN1[XSrc4TpZ4FtdHlic3nncolncWOjboSgdoVlfWO2aX;uJIlvKGKxdHigR3BHNSCjbnSgR3BHM0OPLXnu[JVk\WRiYYDvdJRwe2m|wrC= NF3teIgzPDl5NUK3Oi=>
JJN3 M3LETGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1Xjd|AvOS1zMECg{txO NGHM[GQ4OiCq MW\EUXNQ MWLpcohq[mm2czDj[YxtKGe{b4f0bEB{dGmpaITsfS=> NX2z[W9DOjNzN{izO|g>
XG-1 NFf3bGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zsWFAvOS1zMECg{txO NWDmPXN5PzJiaB?= NXXSS5VRTE2VTx?= NEHrSplqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MXmyN|E4QDN5OB?=
CD138+  M1KyNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLoWFZwOC5zLUGwNEDPxE1? MX[3NkBp NWWxc|A6TE2VTx?= NHz0fW1qdmirYnn0d{Bk\WyuIHfyc5d1cA>? M3m2UlI{OTd6M{e4
XG-1 M{K5XGZ2dmO2aX;uJGF{e2G7 NFTKcmkzNzFyMDFOwG0> M2\ucFI1KGh? MlLLSG1UVw>? NU\IWmJPcW6qaXLpeJMhS0OOMz;NTXAuOc7zIH3SUmEh\XiycnXzd4lwdg>? M{nt[|I{OTd6M{e4
U266 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkL5NE4xOS1zMDFOwG0> NXH0NpB6PDkkgJno MWXEUXNQ NX25[5IzcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NHXX[GIzOjV3MkCwPC=>
CRBN60 M1TjS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPvRlRxOC5yMT2xNEDPxE1? M1X4W|Q56oDLaB?= M1PpdGROW09? NUPT[nFVcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NF\uZWkzOjV3MkCwPC=>
CRNB75 NXnpeXVzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DXPVAvODFvMUCg{txO MnK4OFjjiImq NX\LV4FUTE2VTx?= NVjsW45[cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MVmyNlU2OjByOB?=
MM.1S MlvYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXLNE4xOS1zMDFOwG0> Ml\HOFjjiImq Mlv3SG1UVw>? NFr3V2l{cWewaX\pZ4FvfGy7IHnubIljcXS|IIDyc4xq\mW{YYTpc44h[XRiY3;uZ4VvfHKjdHnvcpMh[XNibH;3JIF{KDBwMEJOwG0> MUGyNVM5QTN{Nx?=
OPM2 M2nmRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXewMlAyNTFyIN88US=> MnXvOFjjiImq Mn[ySG1UVw>? MnLmd4lodmmoaXPhcpRtgSCrbnjpZol1eyCycn;sbYZmemG2aX;uJIF1KGOxbnPlcpRz[XSrb37zJIF{KGyxdzDhd{AxNjBzzszN NUjRSmJrOjF|OEmzNlc>
MM.1S MoL2SpVv[3Srb36gRZN{[Xl? MkDoNVAh|ryP NF\qPJE4OiCq MUDEUXNQ Mli3d4lodmmoaXPhcpRtgSCmZXPy[YF{\XNidHjlJJBzd3SnaX6gcIV3\Wxib3[gR{9GSlEQsjDpd49nd3Kvc9Mg NHjIVXAzOTN6OUOyOy=>
H929 MYXGeY5kfGmxbjDBd5NigQ>? M1fOOlExKM7:TR?= NGj2bo04OiCq NIqySplFVVOR M4G1cpNq\26rZnnjZY51dHliZHXjdoVie2W|IITo[UBxem:2ZXnuJIxmfmWuIH;mJGMwTUKSzsKgbZNw\m:{bYRCpC=> M1TmblIyOzh7M{K3
OPM2 MVLGeY5kfGmxbjDBd5NigQ>? M2\lTVExKM7:TR?= M{m3XlczKGh? M335bWROW09? MVLzbYdvcW[rY3HueIx6KGSnY4LlZZNmeyC2aHWgdJJwfGWrbjDs[ZZmdCCxZjDDM2VDWM7{IHnzc4Zwem2|wrC= NVSzVFd6OjF|OEmzNlc>
CT26 M1LFfWZ2dmO2aX;uJGF{e2G7 Mnm3NU8yOCEQvF2= M3zpRVI1KGh? MlXvdoVlfWOnczD0bIUhdnWvYnXyd{Bw\iCuaY\lJINwdG:waXXzxsA> NYfB[HpbOTl4M{i5O|c>

多くの細胞株試験データを見る場合、クリックしてください

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

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.
細胞試験: [4]
+ 展開
  • 細胞株: Raji, SU-DHL-4 and SU-DHL-10 cell lines
  • 濃度: Dissolved in DMSO, final concentrations 2.5-40 μg/mL
  • 反応時間: 24 or 48 hours
  • 実験の流れ: 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.
    (参考用のみ)
動物試験:[4]
+ 展開
  • 動物モデル: Disseminated lymphoma-bearing SCID mice
  • 製剤: 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.
  • 投薬量: 0.5 mg/kg
  • 投与方法: Injection i.p.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 54 mg/mL (197.62 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます:
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。
3mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 273.24
化学式

C13H11N3O4

CAS No. 19171-19-8
保管
別名 CC-4047

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

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

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

    Is S1567 in the 1% DMSO+30% polyethylene glycol+1% Tween 80 suitable for oral administration?

  • 回答:

    S1567 in 1% DMSO+30% polyethylene glycol+1% Tween 80 is a suspension. This formulation is for oral gavege.

  • 質問2:

    I would like to know if the pomalidomide is racemic or optically active?

  • 回答:

    Our S1567 Pomalidomide is racemic.

TNF-alphaシグナル伝達経路

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID