Ibrutinib (PCI-32765)

For research use only.

Catalog No.S2680

397 publications

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. Ibrutinib is applicable as a Btk ligand in the synthesis of a series of PROTACs including P13I.

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Selleck's Ibrutinib (PCI-32765) has been cited by 397 publications

Purity & Quality Control

Choose Selective Target Protein Ligand Inhibitors

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. Ibrutinib is applicable as a Btk ligand in the synthesis of a series of PROTACs including P13I.
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 MUHGeY5kfGmxbjDhd5NigQ>? M4nJV|EhcA>? NWXl[GRYUW6qaXLpeIlwdiCxZjDoeY1idiCodXzsMYxmdme2aDDCWGsh\XiycnXzd4VlKGmwIGPmPUBk\WyuczD1d4lv\yCIQV2tV5JkfGmmZTDw[ZB1cWSnIHHzJJN2[nO2cnH0[UBi\nSncjC2NEBucW6|IHL5JHRTNU[URWSgRZN{[XoxvJygTWM2OD1yLkWgcm0v NH\nT4MzOTl3OEW0Oy=>
human Pfeiffer cells MULGeY5kfGmxbjDhd5NigQ>? M17VTVczKGh? NX:3d41ZS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWG[naX\m[ZIh[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NkBvVS5? M3nVVFI1QTF3Mkmx
human Ramos cells NHK4SXNHfW6ldHnvckBie3OjeR?= NVvnWIl{OSCq MoPWTY5pcWKrdHnvckBw\iCEdHugbY4hcHWvYX6gVoFud3NiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBRVENvZ3HtcYEzKHCqb4PwbI9zgWyjdHnvckBifCCWeYKxNlE4KGGodHXyJFEhcHJiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{NCCLQ{WwQVE1KG6PLh?= MmH3NlQ6OTV{OUG=
Sf9 cells NIPSWIlHfW6ldHnvckBie3OjeR?= MoL0NUBp NYXpUGJ6UW6qaXLpeIlwdiCxZjDMXW4uSSCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJIFnfGW{IE[wJI1qdnNiYomgWHIuTlKHVDDBd5NigSxiSVO1NF0xNjJizszNMi=> NILDPGEzOTl3OEW0Oy=>
human DOHH2 cells NXXOZ2VrS3m2b4TvfIlkyqCjc4PhfS=> M{\UUVczKGh? M37ISmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGRQUEh{IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIx2dWmwZYPj[Y51KGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNEGg{txONg>? M4LD[|I1QTF3Mkmx
human SU-DHL6 cells NYTJTXhiS3m2b4TvfIlkyqCjc4PhfS=> MmWxO|IhcA>? MYLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTWU1FUEx4IHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIx2dWmwZYPj[Y51KGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNUig{txONg>? MlfZNlQ6OTV{OUG=
human WSU-NHL cells MV;DfZRwfG:6aXRCpIF{e2G7 M2qxTFczKGh? NYrkbW5US3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hX1OXLV7IUEBk\WyuczDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgR4VtdFSrdHXyMWdtdyCudX3pcoV{[2WwdDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlA6KM7:TR?= MU[yOFkyPTJ7MR?=
human Rec1 cells NFLwXlBHfW6ldHnvckBie3OjeR?= MYCyMlUh|ryP M1fQeFYhcA>? NUnFVIVFUW6qaXLpeIlwdiCxZjDMfY4heGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJHJm[zFiY3XscJMh[XRiMj61JJVOKGmwY4XiZZRm\CCob4KgOkBpenNiYomgW4V{fGW{bjDicI91fGmwZzDt[ZRpd2R? NFfPUIYzPTJ{Mki3Oy=>

... 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]
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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]
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  • 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]
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  • Animal Models: MRL-Fas(lpr) lupus model and collagen-induced arthritis model.
  • 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
Smiles NC1=C2C(=NC=N1)[N](N=C2C3=CC=C(OC4=CC=CC=C4)C=C3)C5CCCN(C5)C(=O)C=C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03282396 Not yet recruiting Drug: Ibrutinib CCND1 Positive|CD20 Positive|Mantle Cell Lymphoma M.D. Anderson Cancer Center|National Cancer Institute (NCI) November 30 2020 Phase 2
NCT04294641 Not yet recruiting Drug: Ibrutinib Chronic GVHD National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) May 19 2020 Phase 2
NCT03679624 Suspended Drug: Ibrutinib|Drug: Daratumumab Waldenstrom Macroglobulinemia|Waldenstrom''s Disease|Waldenström; Hypergammaglobulinemia|Waldenstrom''s Macroglobulinemia Recurrent|Waldenstrom''s Macroglobulinemia of Lymph Nodes|Waldenstrom''s Macroglobulinaemia Without Mention of Remission|Waldenstrom''s Macroglobulinemia Refractory Weill Medical College of Cornell University|Janssen Scientific Affairs LLC|Mayo Clinic May 2020 Phase 2
NCT04274738 Not yet recruiting Drug: Mavorixafor|Drug: Ibrutinib Waldenstrom Macroglobulinemia X4 Pharmaceuticals April 2020 Phase 1
NCT03943342 Recruiting Drug: Ibrutinib|Drug: Venetoclax Chronic Lymphocytic Leukemia|Loss of Chromosome 17p Kerry Rogers|National Cancer Institute (NCI)|Janssen Research & Development LLC|Ohio State University Comprehensive Cancer Center March 11 2020 Phase 2
NCT04234061 Not yet recruiting Combination Product: ibrutinib and Tisagenlecleucel Mantle Cell Lymphoma Recurrent Peter MacCallum Cancer Centre Australia|Novartis January 2020 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.

Handling Instructions

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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