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    Ibrutinib (PCI-32765)
    Ibrutinib (PCI-32765)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0643
    CAS #: 936563-96-1Purity ≥98%

    Description: Ibrutinib (formerly PCI32765; trade name Imbruvica), an approved anticancer drug, is a covalent/irreversible and orally bioavailable Brutons tyrosine kinase (Btk) inhibitor with potential anti-cancer activity. It inhibits BTK with an IC50 of 0.5 nM in cell-free assays, and exhibits modest potency against other kinases such as Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc. on November 13th 2013, Ibrutinib was approved by the US FDA for the treatment of mantle cell lymphoma.

    References: Proc Natl Acad Sci U S A. 2010;107(29):13075-80; Blood. 2011;117(23):6287-96; Blood. 2012;119(5):1182-9. 

    Related CAS: 936563-87-0 (Ibrutinib Racemate); 1599432-18-4 (Ibrutinib-biotin); 143900-44-1 (Ibrutinib Interm 0441); 1710768-30-1 (Ibrutinib-MPEA); 1553977-17-5 (Ibrutinib D5)

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    Molecular Weight (MW)440.5
    FormulaC25H24N6O2
    CAS No.936563-96-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 88 mg/mL (199.8 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)2% DMSO+Castor oil: 10 mg/mL
    SynonymsPCI-32765; PCI-32765, Ibrutinib, PCI 32765, trade name: Imbruvica 

    Chemical Name: (R)-1-(3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one.

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


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    In Vitro

    In vitro activity: 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. 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. 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.


    Kinase Assay: 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 Assay: 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.

    In VivoMRL-Fas(lpr) lupus model and collagen-induced arthritis model.
    Animal modelMale 5-week-old BALB-nu/nu with HPAC cells
    Formulation & DosageDissolved in DMSO; 50 mg/kg; Oral gavage
    References

    Proc Natl Acad Sci U S A. 2010 Jul 20;107(29):13075-80; Blood. 2011 Jun 9;117(23):6287-96; Blood. 2012 Feb 2;119(5):1182-9. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Ibrutinib (PCI-32765)


    Ibrutinib (PCI-32765)
    Ibrutinib (PCI-32765)


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