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 NU[3VplHS3m2b4TvfIlkcXS7IFHzd4F6 M3jVfFExKM7:TR?= NEfBSlYzPCCq MVLwc5RmdnSueTDheYdu\W62czDkbZJm[3RiYX7kJIlv\Gm{ZXP0JG1OKGOnbHygb4ltdGmwZzDifUBUSVJ? NI\m[GwzPjN|OEK3Ny=>
J-CD38 MnK4R5l1d3SxeHnjbZR6KEG|c3H5 M4PvOlExKM7:TR?= NFvEc20zPCCq NYj3UJZJeG:2ZX70cJkh[XWpbXXueJMh\Gm{ZXP0JIFv\CCrbnTpdoVkfCCPTTDj[YxtKGurbHzpcoch[nliU1HS MnjoNlY{Ozh{N{O=
R-CD38 NXuxbY9KS3m2b4TvfIlkcXS7IFHzd4F6 M2foRVExKM7:TR?= NGTyUFUzPCCq M4XPWJBwfGWwdHz5JIF2\22nboTzJIRqemWldDDhcoQhcW6maYLlZ5QhVU1iY3XscEBscWyuaX7nJIJ6KFODUh?= NGXlOY0zPjN|OEK3Ny=>
BC-3 M3i2Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkSwN|kuOTJ3MDDuUS=> Mn\mOUBl NIjDcWhFVVORwrC= M4nnfGlEPTB;MUC3JI5ONCCrbnjpZol1eyClZXzsJGlEPTB;MUC3JI5ONCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MV6yOlEyQTl|OR?=
BCBL-1 NXjJUGNRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHZRpJ4OzlvMUK1NEBvVQ>? MV61JIQ> NGjJZodFVVORwrC= NFPDOFBKSzVyPUe0JI5ONCCrbnjpZol1eyClZXzsJJZq[WKrbHn0fUBld3OnIHTldIVv\GWwdHz5 NW\GTFhOOjZzMUm5N|k>
JSC-1 MmjaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXmzPU0yOjVyIH7N NUGyPHZFPSCm NV[3S4R1TE2VT9Mg MkDvTWM2OD1|NDDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NXe3VnViOjZzMUm5N|k>
VG-1 M37VfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV[zPU0yOjVyIH7N M4TPW|Uh\A>? NVfENZFNTE2VT9Mg NVW0cGVTUUN3ME2xNFEhdk1uIHnubIljcXS|IHPlcIwhfmmjYnnsbZR6KGSxc3Wg[IVx\W6mZX70cJk> NHOzZ3MzPjFzOUmzPS=>
UMPEL-1 MknxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVyzPU0yOjVyIH7N MnPxOUBl Moe3SG1UV8Li M3\jNGlEPTB;M{Kgcm0tKGmwaHnibZR{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= M{PDNVI3OTF7OUO5
UMPEL-3 M3f0Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPRXnY6OzlvMUK1NEBvVQ>? M3S0OlUh\A>? NVvpWINMTE2VT9Mg NFPmeopKSzVyPUGxNUBvVSxiaX7obYJqfHNiY3XscEB3cWGkaXzpeJkh\G:|ZTDk[ZBmdmSnboTsfS=> NXe2UpZIOjZzMUm5N|k>
BC-1 Ml;VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17DRlM6NTF{NUCgcm0> NUXRRVFIPSCm MUDEUXNQyqB? MXzJR|UxRTd2NDDuUUwhcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MVWyOlEyQTl|OR?=
BCP-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXrfZNQOzlvMUK1NEBvVQ>? Mkn3OUBl Ml;DSG1UV8Li MlPkTWM2OD1|OU[gcm0tKGmwaHnibZR{KGOnbHygeoli[mmuaYT5JIRwe2ViZHXw[Y5l\W62bIm= NX;MemVmOjZzMUm5N|k>
APK-1 M1K0T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33r[FM6NTF{NUCgcm0> NIHPWHY2KGR? MUXEUXNQyqB? NELnSHlKSzVyPUKyOkBvVSxiaX7obYJqfHNiY3XscEB3cWGkaXzpeJkh\G:|ZTDk[ZBmdmSnboTsfS=> NWXyVYNDOjZzMUm5N|k>
RPMI8226  NUTD[mVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTweGQ2OC5yMT21NEDPxE1? NWTZclVkPDhiaB?= MmLkSG1UV8Li NF3JXVlKSzVyPUig{txO NETNcm0zPjB7N{i3Ni=>
OPM2  NE[ye|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;KN3ExNjBzLUWwJO69VQ>? NYDEN5BVPDhiaB?= MkDKSG1UV8Li MWnJR|UxRTFyIN88US=> MX2yOlA6Pzh5Mh?=
RPMI8226  MoPJSpVv[3Srb36gRZN{[Xl? Mnz1NVAh|ryP NHPEUFg1QCCq NHzZfHhFVVORwrC= NUS3UnlWe3S{ZX7neIhmdnNiY4n0c5Bt[XOvaXOtcpVkdGWjcjDzbJV1fGyrbnegc4YhdVSRUjDhcoQheC2vVF;SJJBzd3SnaX6= MY[yOlA6Pzh5Mh?=
OPM2  NXnnNJdvTnWwY4Tpc44hSXO|YYm= MmPBNVAh|ryP NWC3[GJRPDhiaB?= NGGycJpFVVORwrC= NHTEUHN{fHKnbnf0bIVveyCleYTvdIxie22rYz3ueYNt\WG{IIPoeZR1dGmwZzDv[kBuXE:UIHHu[EBxNW2WT2KgdJJwfGWrbh?= NIrJblIzPjB7N{i3Ni=>
RPMI8226 MlL5SpVv[3Srb36gRZN{[Xl? M1u3eFAvOS1zMDFOwG0> NV;KUW57PCCq Moi2SG1UV8Li MV;pcoNz\WG|ZYOgWmVITiCvUl7BJIV5eHKnc4Ppc44> NEXscZgzPTB3M{m5NC=>
SH-SY5Y  MmXwRZBweHSxc3nzJGF{e2G7 NEPLV2YzPcLizsznM41N MUOxxsBp M{i1OYNifXOnczDzeIF1cXO2aXPhcIx6KHOrZ37p[olk[W62IILl[JVkfGmxbjDpckBjd3SqIFPQSk0h[W6mIFPQSktEVS2rbnT1Z4VlKGGyb4D0c5Nqe8Li MXKyOFk4PTJ5Nh?=
JJN3 MlTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTlNE4yNTFyMDFOwG0> NFjRV5g4OiCq MV\EUXNQ MX\pcohq[mm2czDj[YxtKGe{b4f0bEB{dGmpaITsfS=> NFP3ZXMzOzF5OEO3PC=>
XG-1 M{H6XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonoNE4yNTFyMDFOwG0> MUS3NkBp NETyVm9FVVOR M4DWRolvcGmkaYTzJINmdGxiZ4Lve5Rp NXyxbWt3OjNzN{izO|g>
CD138+  NVXxS2FrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfnSGwxNjFvMUCwJO69VQ>? M4HOVVczKGh? M13l[mROW09? MlfwbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NF3NSWozOzF5OEO3PC=>
XG-1 MUDGeY5kfGmxbjDBd5NigQ>? MX:yM|ExOCEQvF2= NX7OPVhUOjRiaB?= MULEUXNQ MUfpcohq[mm2czDDR2w{N02LUD2x{tEhdVKQQTDlfJBz\XO|aX;u MlnFNlMyPzh|N{i=
U266 M2HheWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHhNE4xOS1zMDFOwG0> MXi0PQKBkWh? NVr4fYl{TE2VTx?= M1nHNolvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> MWCyNlU2OjByOB?=
CRBN60 NYDjSZU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\lNE4xOS1zMDFOwG0> MVu0PQKBkWh? NGXRVldFVVOR M3;Bc4lvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> M{DHWVIzPTV{MEC4
CRNB75 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2W1SFAvODFvMUCg{txO NX[yfYFXPDkkgJno MUjEUXNQ NYTXOHZ3cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? MXWyNlU2OjByOB?=
MM.1S NYm5bZJJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoH5NE4xOS1zMDFOwG0> M3zi[VQ56oDLaB?= M4DpS2ROW09? NFHIeZp{cWewaX\pZ4FvfGy7IHnubIljcXS|IIDyc4xq\mW{YYTpc44h[XRiY3;uZ4VvfHKjdHnvcpMh[XNibH;3JIF{KDBwMEJOwG0> MkPiNlE{QDl|Mke=
OPM2 NXfWdnFDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fYV|AvODFvMUCg{txO NGS4Z2Y1QOLCiXi= NVrmT25[TE2VTx?= MXrzbYdvcW[rY3HueIx6KGmwaHnibZR{KHC{b3zp[oVz[XSrb36gZZQh[2:wY3XueJJifGmxboOgZZMhdG:5IHHzJFAvODIQvF2= MkXqNlE{QDl|Mke=
MM.1S MonJSpVv[3Srb36gRZN{[Xl? NH\qTFcyOCEQvF2= M{CxUlczKGh? MnnFSG1UVw>? M{H2[5Nq\26rZnnjZY51dHliZHXjdoVie2W|IITo[UBxem:2ZXnuJIxmfmWuIH;mJGMwTUKSzsKgbZNw\m:{bYRCpC=> NVTnZ5pJOjF|OEmzNlc>
H929 MUfGeY5kfGmxbjDBd5NigQ>? NHLZ[osyOCEQvF2= MknBO|IhcA>? NFmw[4pFVVOR M374UJNq\26rZnnjZY51dHliZHXjdoVie2W|IITo[UBxem:2ZXnuJIxmfmWuIH;mJGMwTUKSzsKgbZNw\m:{bYRCpC=> M3\uS|IyOzh7M{K3
OPM2 MkLMSpVv[3Srb36gRZN{[Xl? MVSxNEDPxE1? M4fISVczKGh? NV7DZXY1TE2VTx?= Mni0d4lodmmoaXPhcpRtgSCmZXPy[YF{\XNidHjlJJBzd3SnaX6gcIV3\Wxib3[gR{9GSlEQsjDpd49nd3Kvc9Mg Mme4NlE{QDl|Mke=
CT26 NGC4bZpHfW6ldHnvckBCe3OjeR?= MmmwNU8yOCEQvF2= Mn[5NlQhcA>? M1vibZJm\HWlZYOgeIhmKG63bXLldpMhd2ZibHn2[UBkd2yxbnnld:Kh NV[xc5NzOTl4M{i5O|c>

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

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(文献ではなく、Selleckの実験によるデータ):
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
in solvent
別名 CC-4047

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    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

貯蔵液を準備するために必要な希釈率を計算してください。Selleck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 ( 入力 出力 )

  • 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

質量 濃度 体積 分子量

臨床試験

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
NCT01178281 Active not recruiting Primary Myelofibrosis Celgene September 8 2010 Phase 3
NCT02807454 Active not recruiting Multiple Myeloma Celgene July 7 2016 Phase 2
NCT02400242 Active not recruiting Multiple Myeloma Celgene May 7 2015 Phase 1
NCT01734928 Active not recruiting Multiple Myeloma Celgene January 7 2013 Phase 3

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

TNF-alpha Inhibitors with Unique Features

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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