Ibrutinib (PCI-32765)

Catalog No.S2680

Ibrutinib (PCI-32765) Chemical Structure

Molecular Weight(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.

Size Price Stock Quantity  
In DMSO USD 272 In stock
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USD 320 In stock
USD 970 In stock
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Cited by 59 Publications

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Biological Activity

Description 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.
Targets
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
In vitro

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]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 cells M2LSTmZ2dmO2aX;uJIF{e2G7 Mn\NNUBp NFHLO2xKdmirYnn0bY9vKG:oIHj1cYFvKG[3bHytcIVv\3SqIFLUT{BmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IIXzbY5oKE[DTT3TdoN1cWSnIIDldJRq\GViYYOgd5Vje3S{YYTlJIFnfGW{IE[wJI1qdnNiYomgWHIuTlKHVDDBd5Nige,:jDDJR|UxRTBwNTDuUU4> MlPkNlE6PTh3NEe=
human Pfeiffer cells NFTYNGRHfW6ldHnvckBie3OjeR?= MWi3NkBp NFH3dI9EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBR\mWrZn\ldkBk\WyuczDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCudX3pcoV{[2WwdDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yJI5ONg>? NGC2fIkzPDlzNUK5NS=>
human Ramos cells MXrGeY5kfGmxbjDhd5NigQ>? MX6xJIg> NXG2OWFIUW6qaXLpeIlwdiCxZjDCeIshcW5iaIXtZY4hWmGvb4OgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCSTFOt[4FudWF{IIDoc5NxcG:{eXzheIlwdiCjdDDUfZIyOjF5IHHmeIVzKDFiaIKgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m|LDDJR|UxRTF2IH7NMi=> NGHDeXEzPDlzNUK5NS=>
Sf9 cells M1\TOmZ2dmO2aX;uJIF{e2G7 MY[xJIg> MkmzTY5pcWKrdHnvckBw\iCOWV6tRUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IHHmeIVzKDZyIH3pcpMh[nliVGKtSnJGXCCDc4PhfUwhUUN3ME2wMlIh|ryPLh?= NUDMcXdHOjF7NUi1OFc>
human DOHH2 cells Mom4R5l1d3SxeHnjxsBie3OjeR?= NXL4SoRPPzJiaB?= NYnWemFqS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hTE:KSEKgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60NUDPxE1w NUfMcZVbOjR7MUWyPVE>
human SU-DHL6 cells MYDDfZRwfG:6aXRCpIF{e2G7 NXnqe|ZmPzJiaB?= NHK0cmpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUXS2GSFy2JINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGy3bXnu[ZNk\W62IHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOVgh|ryPLh?= MkexNlQ6OTV{OUG=
human WSU-NHL cells MVjDfZRwfG:6aXRCpIF{e2G7 NIfBR2I4OiCq NGW4dIpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBYW1VvTljMJINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGy3bXnu[ZNk\W62IHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNFkh|ryP NV\hbXBkOjR7MUWyPVE>
human Rec1 cells NHGyOoZHfW6ldHnvckBie3OjeR?= NGPYO2IzNjVizszN M1rOSVYhcA>? MlTrTY5pcWKrdHnvckBw\iCOeX6gdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIGLlZ|Eh[2WubIOgZZQhOi53IIXNJIlv[3WkYYTl[EBnd3JiNjDodpMh[nliV3XzeIVzdiCkbH;0eIlv\yCvZYToc4Q> MV[yOVIzOjh5Nx?=

... Click to View More Cell Line Experimental Data
Assay
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
In vivo 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]

Protocol

Kinase Assay:

[1]
+ Expand

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.
Cell Research:

[2]
+ Expand
  • Cell lines: Chronic lymphocytic leukemia (CLL) cells
  • Concentrations: 0.01-100 μM
  • Incubation Time: 48 hours
  • Method:

    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.


    (Only for Reference)
Animal Research:

[1]
+ Expand
  • Animal Models: MRL-Fas(lpr) lupus model and collagen-induced arthritis model.
  • Formulation: Ibrutinib is dissolved in DMSO.
  • Dosages: ≤50 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 88 mg/mL (199.77 mM)
Ethanol 45 mg/mL (102.15 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing. 		10mg/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 440.5
Formula

C25H24N6O2
CAS No. 936563-96-1
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

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

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:

    How to reconstitute the compound S2680 for in vivo studies?

  • Answer:

    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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID