Ibrutinib (PCI-32765)

製品コードS2680

Ibrutinib (PCI-32765)化学構造

分子量(MW)：440.5

Ibrutinib (PCI-32765) is a potent and highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM in cell-free assays, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc.

サイズ 価格(税別)  
In DMSO JPY 47100
JPY 30200
JPY 55100
JPY 163000
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バルク問合せ

文献中Selleckの製品使用例(88)

製品安全説明書

BTK阻害剤の選択性比較

生物活性

製品説明 Ibrutinib (PCI-32765) is a potent and highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM in cell-free assays, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc.
ターゲット
BTK [1]
(Cell-free assay)		 BLK [1]
(Cell-free assay)		 Bmx [1]
(Cell-free assay)		 CSK [1]
(Cell-free assay)		 FGR [1]
(Cell-free assay)
0.5 nM 0.5 nM 0.8 nM 2.3 nM 2.3 nM
体外試験

Ibrutinib shows the potent and irreversible inhibitory effect and selectivity for Btk enzymatic activity. In BCR pathway-activated DOHH2 cell line, Ibrutinib inhibits autophosphorylation of Btk, phosphorylation of Btk's physiological substrate PLCγ, and phosphorylation of further downstream kinase, ERK with IC50 of 11 nM, 29 nM and 13 nM, respectively. [1] Ibrutinib exhibits a significant dose-dependent and time-dependent induction of cytotoxicity in chronic lymphocytic leukemia (CLL) cells. In addition, Ibrutinib induces cell death depending on caspase pathway activation and antagonizes the ability of CLL cells to proliferate after TLR signaling. [2] A recent study shows that Ibrutinib inhibits BCR-activated primary B cell proliferation with IC50 of 8 nM and results in inhibition of TNFα, IL-1β and IL-6 production in primary monocytes with IC50 of 2.6 nM, 0.5 nM and 3.9 nM, respectively. [3]
細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 cells Mme2SpVv[3Srb36gZZN{[Xl? NUHJSodbOSCq MUjJcohq[mm2aX;uJI9nKGi3bXHuJIZ2dGxvbHXu[5RpKEKWSzDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{KHW|aX7nJGZCVS2VcnP0bYRmKHCncITp[IUh[XNic4Xid5Rz[XSnIHHmeIVzKDZyIH3pcpMh[nliVGKtSnJGXCCDc4Phfg+9lCCLQ{WwQVAvPSCwTT6= MY[yNVk2QDV2Nx?=
human Pfeiffer cells M17MWWZ2dmO2aX;uJIF{e2G7 M336OFczKGh? NWXDT5BXS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWG[naX\m[ZIh[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NkBvVS5? Mn;aNlQ6OTV{OUG=
human Ramos cells MlntSpVv[3Srb36gZZN{[Xl? M1PhXVEhcA>? M17ndGlvcGmkaYTpc44hd2ZiQoTrJIlvKGi3bXHuJHJidW:|IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhWEyFLXfhcY1iOiCyaH;zdIhwenmuYYTpc44h[XRiVInyNVIyPyCjZoTldkAyKGi{IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqeyxiSVO1NF0yPCCwTT6= NHHN[IIzPDlzNUK5NS=>
Sf9 cells M3nUU2Z2dmO2aX;uJIF{e2G7 M17SdVEhcA>? MXnJcohq[mm2aX;uJI9nKEy\Tj3BJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiYX\0[ZIhPjBibXnud{BjgSCWUj3GVmVVKEG|c3H5MEBKSzVyPUCuNkDPxE1w NEfwdYwzOTl3OEW0Oy=>
human DOHH2 cells M{\UXWN6fG:2b4jpZ:Kh[XO|YYm= NV;pZpB1PzJiaB?= NYnGXWdJS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTE:KSEKgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60NUDPxE1w NHj3WXQzPDlzNUK5NS=>
human SU-DHL6 cells NWjG[4ZHS3m2b4TvfIlkyqCjc4PhfS=> MW[3NkBp MkHhR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV3UuTEiONjDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{BtfW2rbnXzZ4VvfCClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkW4JO69VS5? MmXuNlQ6OTV{OUG=
human WSU-NHL cells MVfDfZRwfG:6aXRCpIF{e2G7 NXvPUXRLPzJiaB?= M3LRfGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHdUXS2QSFygZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6wPUDPxE1? M3ywblI1QTF3Mkmx
human Rec1 cells NUi1WHRVTnWwY4Tpc44h[XO|YYm= NUfab49GOi53IN88US=> M{CwfFYhcA>? MkTaTY5pcWKrdHnvckBw\iCOeX6gdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIGLlZ|Eh[2WubIOgZZQhOi53IIXNJIlv[3WkYYTl[EBnd3JiNjDodpMh[nliV3XzeIVzdiCkbH;0eIlv\yCvZYToc4Q> NHq4WWozPTJ{Mki3Oy=>

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アッセイ
Methods Test Index PMID
Western blot
pEGFR(Tyr1068) / EGFR; 

PubMed: 28061447     


Ibrutinib inhibitory effects on EGFRY1068 auto-phosphorylation in the HCC827 cell line at different time points by removal of drug after 4 h pretreatment.

pBTK / pPLCγ2 / pAKT / pERK / pJNK; 

PubMed: 23940282     


Mino (left panel) or Jeko1 (right panel) cells pretreated with vehicle or ibrutinib 10, 100, or 1000 nM were either stimulated with anti-IgM, CXCL12, or CXCL13 or treated with medium (Med) for 15 minutes and then immunoblotted for pBTK, pPLCγ2, pAKT, pERK, and pJNK.

28061447 23940282
Immunofluorescence
CD11b; 

PubMed: 30231870     


BV2 microglial cells were pretreated with ibrutinib (1 μM) or vehicle (1% DMSO) for 30 min, followed by treatment with LPS (1 μg/ml) or PBS for 5.5 h and immunostaining with an anti-CD11b antibody. Scale bar = 20 μm.

COX-2; 

PubMed: 30231870     


BV2 microglial cells were treated with vehicle (1% DMSO) or ibrutinib (1 μM) for 30 min, followed by PBS or LPS (1 μg/ml) for 5.5 h, and immunocytochemistry was conducted with anti-CD11b and anti-COX-2 antibodies. 

30231870
ELISA
hTNFα; 

PubMed: 26627823     


PBMs were isolated and pretreated with 1, 5, or 10 μm ibrutinib (IB) or left untreated (UT, −). Pretreated PBMs were incubated for 24 h in 96-well plates precoated without (PBS) or with 10 μg/ml whole human IgG. Cleared supernatants were collected and analyzed by ELISA for TNFα (n = 3).

IL-10; 

PubMed: 27792904     


LMP2A-negative (vector.1/.2) and -positive (express LMP2A) B cell lines were incubated in the absence or presence of increasing concentrations of Ibrutinib for 24 hours and supernatants were isolated for analysis using an IL-10 ELISA.

26627823 27792904
体内試験 In a collagen-induced arthritis model, Ibrutinib significantly reduces clinical arthritis scores reflecting paw swelling and joint inflammation by inhibiting B-cell activation. In a MRL-Fas(lpr) lupus model, Ibrutinib reduces renal disease and autoantibody production. [1] In an adoptive transfer TCL1 mouse model of CLL, Ibrutinib (25 mg/kg/day) causes a transient early lymphocytosis, and delays CLL disease progression. [4]

お薦めの試験操作（参考用のみ）

キナーゼ試験：

[1]
+ 展開

Kinase Assays :

In vitro kinase IC50 values are measured using 33P filtration binding assay after 1 hour incubation of kinase, 33P-ATP, Ibrutinib, and substrate [0.2 mg/mL poly(EY)(4:1]. Assays are performed at Reaction Biology.
細胞試験：

[2]
+ 展開
  • 細胞株： Chronic lymphocytic leukemia (CLL) cells
  • 濃度： 0.01-100 μM
  • 反応時間： 48 hours
  • 実験の流れ：

    MTT (3'[4,5-dimethylthiazol-2-yl]-2,5-diphenyl-tetrazolium bromide) assays are performed to determine cytotoxicity. Briefly, cells (CLL B cells or healthy volunteer T cells or NK cells) are incubated for 48 hours with different concentrations of Ibrutinib, or vehicle control. MTT reagent is then added, and plates are incubated for an additional 20 hours before washing with protamine sulfate in phosphate-buffered saline. Dimethyl sulfoxide is added, and absorbance is measured by spectrophotometry at 540 nm in a Labsystems plate reader. Cell viability is also measured at various time points with the use of annexin/PI flow cytometry. Data are analyzed with Expo-ADC32 software package. Results are expressed as the percentage of total positive cells over untreated control. Experiments examining caspase-dependent apoptosis includes the addition of 100μM Z-VAD.


    (参考用のみ)
動物試験：

[1]
+ 展開
  • 動物モデル： MRL-Fas(lpr) lupus model and collagen-induced arthritis model.
  • 製剤： Ibrutinib is dissolved in DMSO.
  • 投薬量： ≤50 mg/kg
  • 投与方法： Administered via p.o.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 88 mg/mL (199.77 mM)
Ethanol 45 mg/mL (102.15 mM)
Water 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):
5% DMSO+30% PEG 300+5% 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。 		10mg/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 440.5
化学式

C25H24N6O2
CAS No. 936563-96-1
保管 粉
in solvent
別名 N/A

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
NCT03873493 Not yet recruiting Leukemia|T-cell Prolymphocytic Leukemia (T-PLL)|Cancer AbbVie June 6 2019 Phase 2
NCT03873493 Not yet recruiting Leukemia|T-cell Prolymphocytic Leukemia (T-PLL)|Cancer AbbVie June 6 2019 Phase 2
NCT03514017 Not yet recruiting Chronic Lymphocytic Leukemia H. Lee Moffitt Cancer Center and Research Institute|Merck Sharp & Dohme Corp.|Janssen Scientific Affairs LLC May 2019 Phase 2
NCT03514017 Not yet recruiting Chronic Lymphocytic Leukemia H. Lee Moffitt Cancer Center and Research Institute|Merck Sharp & Dohme Corp.|Janssen Scientific Affairs LLC May 2019 Phase 2
NCT03697512 Not yet recruiting Marginal Zone Lymphoma|Nodal Marginal Zone Lymphoma|Splenic Marginal Zone Lymphoma International Extranodal Lymphoma Study Group (IELSG) April 15 2019 Phase 2
NCT03513562 Not yet recruiting Chronic Lymphocytic Leukemia|Ibrutinib Resistance Ohio State University Comprehensive Cancer Center|National Cancer Institute (NCI) April 30 2019 Phase 2

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：

    How to reconstitute the compound S2680 for in vivo studies?

  • 回答：

    For in vivo study, we suggest to use 5% DMSO+30% PEG 300+5% Tween 80+ddH2O up to 10mg/ml.

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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