1. Protein Tyrosine Kinase/RTK
    PROTAC
  2. Btk
    Ligand for Target Protein for PROTAC
  3. Ibrutinib

Ibrutinib (Synonyms: PCI-32765)

Cat. No.: HY-10997 Purity: 99.93%
Handling Instructions

Ibrutinib (PCI-32765) est un Btk inhibiteur sélectif et irréversible avec un IC50 de 0,5 nM.

Ibrutinib (PCI-32765) ist ein selektiver, irreversibler Btk-Inhibitor mit einem IC50 -Wert von 0,5 nM.

Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.

For research use only. We do not sell to patients.

Ibrutinib Chemical Structure

Ibrutinib Chemical Structure

CAS No. : 936563-96-1

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10 mM * 1 mL in DMSO USD 66 In-stock
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Customer Review

Based on 55 publication(s) in Google Scholar

Other Forms of Ibrutinib:

Top Publications Citing Use of Products

Publications Citing Use of MCE Ibrutinib

    Ibrutinib purchased from MCE. Usage Cited in: Oncotarget. 2015 Oct 13;6(31):31313-22.

    Effect of Ibrutinib on EGFR wt/mutant NSCLCs. Ibrutinib effects on wt EGFR and mutant EGFR- mediated signaling pathways. The results demonstrate that Ibrutinib potently inhibits both EGFR wt/mutant auto-phosphorylation at Y1068.

    Ibrutinib purchased from MCE. Usage Cited in: Oncotarget. 2015 Oct 13;6(31):31313-22.

    Effect of Ibrutinib, WZ4002, AZD9291 and CO1686 on EGFR phosphorylation of tyrosines 1068 and 1173 in EGFR-dependent cancer cell lines.

    Ibrutinib purchased from MCE. Usage Cited in: Mol Cell Proteomics. 2012 Jun;11(6):M112.017764.

    Btk protein tyrosine kinase is involved in TSLP signaling. Western blotting analysis is performed to demonstrate the roles of Btk in TSLP-induced Stat3 and Stat5 phosphorylation. Exponentially growing Ba/F3-IT cells are pretreated with 0.1% DMSO or 1 μM PCI-32765 or 10 μM PCI-32765 for 1 h at 37 °C and then are stimulated with TSLP for the indicated times at 37 °C. The phosphorylation of Btk, Stat3, and Stat5a is probed with phosphospecific antibodies against p-Btk (Y551), p-Stat3 (Y705), and p-

    Ibrutinib purchased from MCE. Usage Cited in: Br J Haematol. 2015 Jul;170(1):134-8.

    Treatment of CXCR4WT and CXCR4S338X BCWM.1 and MWCL-1 cells with Ibrutinib or CAL-101 induced caspase-3 and PARP cleavage at 6 h. Caspase-3 and PAPR cleavage following Ibrutinib (IB), CAL-101 (ID), ABT-199 (ABT), in the presence of absence of CXCL12 (SDF) and AMD3100 (AMD).

    Ibrutinib purchased from MCE. Usage Cited in: Oncotarget. 2016 Oct 25;7(43):69760-69769.

    Ibrutinib and WZ4002 inhibitory effects on EGFRY1068 auto-phosphorylation in the H1975 cell line at different time points by removal of drug after 4 h pretreatment

    Ibrutinib purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2017 Sep 25;36(1):132.

    The effects of Ibrutinib on the expression levels of cell cycle-related protein. U87 and U251 cells are treated with Ibrutinib for 12 h. The protein extracts are examined using Western blot analysis with the indicated antibodies.

    Ibrutinib purchased from MCE. Usage Cited in: Blood. 2016 Jun 23;127(25):3237-52.

    Ibrutinib binds to the ATP-binding pocketof HCK and blocks ATP binding. Results from kinase active-site inhibition assaysutilizing an ATP-BTN probe that is used to pull downactive kinases in the presence of Ibrutinib, CC-292, or A419259 in lysates from BCWM.1 WM cells.

    Ibrutinib purchased from MCE. Usage Cited in: Signal Transduct Target Ther. 2017 Oct 27;2:17051.

    BTK inhibitors suppress phosphorylation of STAT3 in JVM-3 cells and CLL patient cells. Cells are treated with varying concentrations of Ibrutinib for indicated time periods and western blotting is performed.

    Ibrutinib purchased from MCE. Usage Cited in: Patent. US20160222465A1.

    Impact of Ibrutinib on p-AKT, ERK and BTK expression following SDF-1a stimulation of plenti-GFP vector, CXCR4WT and CXCR4S338X expressing BCWM.1 cells.

    Ibrutinib purchased from MCE. Usage Cited in: The Graduate School College of Medicine. The Pennsylvania State University. 2015 Jul.

    JVM-3 cells are treated with BTK inhibitor, Ibrutinib for 6 hours and Western blotting is performed to determine protein levels.

    Ibrutinib purchased from MCE. Usage Cited in: J Neuroimmune Pharmacol. 2019 Sep;14(3):448-461.

    Representative confocal microscopy images of BV2 cells incubated with 1 μM of CC-292 or ibrutinib for 2 h followed by incubation with pHrodo zymosan particles for 1 h.

    Ibrutinib purchased from MCE. Usage Cited in: J Neuroimmune Pharmacol. 2019 Sep;14(3):448-461.

    Representative confocal microscopy images of human monocyte-derived macrophages incubated with 1 μM of CC-292 or ibrutinib for 24 h followed by incubation with pHrodo zymosan particles for 1 h.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM[1].

    IC50 & Target

    IC50: 0.5 nM (Btk)

    In Vitro

    Ibrutinib (PCI-32765) selectively inhibits B-cell signaling and activation. It inhibits autophosphorylation of Btk (IC50=11 nM), phosphorylation of Btk's physiological substrate PLCγ (IC50=29 nM), and phosphorylation of a further downstream kinase, ERK (IC50=13 nM)[1].
    Ibrutinib (PCI-32765) inhibits BCR-activated primary B cell proliferation (IC50=8 nM). Following FcγR stimulation, Ibrutinib (PCI-32765) inhibits TNFα, IL-1β and IL-6 production in primary monocytes (IC50=2.6, 0.5, 3.9 nM, respectively)[3].
    Ibrutinib binds C481 (Cysteine481) of BTK with an ideal IC50 of 0.5 nM. Ibrutinib cannot form a covalent bond with the hydroxyl group of serine, C481S mutation increases the IC50 against BTK-C481S phosphorylation from 2.2 nM to 1 μM[4].

    In Vivo

    Ibrutinib (PCI-32765) (3.125-50 mg/kg, p.o.) reduces the level of circulating autoantibodies and completely suppresses disease in mice with collagen-induced arthritis. Ibrutinib (PCI-32765) inhibits autoantibody production and the development of kidney disease in the MRL-Fas(lpr) lupus model. Ibrutinib (PCI-32765) (3.125-50 mg/kg, p.o.) reduces renal disease and autoantibody production in MRL-Fas(lpr) mice[1]. Ibrutinib (PCI-32765) (0.1 μM) inhibits activation-induced proliferation of CLL cells, induces selective cytotoxicity in B cells compared with T cells, but alters activation induced T-cell cytokine production[2]. Ibrutinib (PCI-32765) dose-dependently and potently reverses arthritic inflammation in a therapeutic CIA model with an ED50 of 2.6 mg/kg/day. Ibrutinib (PCI-32765) also prevents clinical arthritis in CAIA models[3].

    Clinical Trial
    Molecular Weight

    440.50

    Formula

    C₂₅H₂₄N₆O₂

    CAS No.

    936563-96-1

    SMILES

    C=CC(N1C[[email protected]](N2N=C(C3=CC=C(OC4=CC=CC=C4)C=C3)C5=C(N)N=CN=C52)CCC1)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 30 mg/mL (68.10 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2701 mL 11.3507 mL 22.7015 mL
    5 mM 0.4540 mL 2.2701 mL 4.5403 mL
    10 mM 0.2270 mL 1.1351 mL 2.2701 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (5.68 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [3]

    Primary human B cells are isolated from peripheral blood mononuclear cell using human Miltenyl human B cell Isolation Kit II. In 0.2 mL RPMI plus 10% FBS, 100,000 B cells are treated with Ibrutinib (PCI-32765) (0.3 nM-10 μM) in triplicate wells or vehicle control in 0.1% DMSO final concentration for 30 minutes at 37°C, 5% CO2, then cells are stimulated with 10 μg/mL anti-IgM F(ab')2, 5 μg/mL anti-CD3/CD28 as a negative control or 0.5 μg/mL PMA (Phorbal 12-myristate 13-acetate) as a positive control. B cells are stimulated for 72 hours at 37°C, 5% CO2. Proliferation is measured with Cell Titer Glo reagent and measured on a luminometer.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    Male DBA1/1OlaHsd mice are injected on days 0 and 21 with Freunds' Complete Adjuvant containing bovine type II collagen. On days 21 to 35, mice are randomized into treatment groups when the average clinical score of each animal is 1.5 (in a scale of 5). Ibrutinib (PCI-32765) treatment (1.56-12.5 mg/kg, p.o.) is initiated following enrollment and continues for 18 days. Clinical scores are given to each mouse daily for each paw. Clinical score assessment is made using the following criteria: 0=normal; 1=one hind paw or fore paw joint affected or minimal diffuse erythema and swelling; 2=two hind or fore paw joints affected or mild diffuse erythema and swelling; 3=three hind or fore paw joints affected or moderate diffuse erythema and swelling; 4=marked diffuse erythema and swelling or four digit joints affected; 5=severe diffuse erythema and severe swelling of entire paw, unable to flex digits.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.93%

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    Keywords:

    IbrutinibPCI-32765PCI32765PCI 32765BtkLigand for Target Protein for PROTACBruton tyrosine kinaseTarget Protein-binding MoietyInhibitorinhibitorinhibit

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