1. Protein Tyrosine Kinase/RTK
  2. Btk

PCI-32765 (Synonyms: Ibrutinib; PCI32765; PCI 32765)

Cat. No.: HY-10997 Purity: 99.87% ee.: 99.50%
Data Sheet SDS Handling Instructions

PCI-32765 is a selective, irreversible Btk inhibitor with IC50 value of 0.5 nM.

For research use only. We do not sell to patients.
PCI-32765 Chemical Structure

PCI-32765 Chemical Structure

CAS No. : 936563-96-1

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10 mM * 1 mL in DMSO $362 In-stock
100 mg $329 In-stock
250 mg $549 In-stock
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Other Forms of PCI-32765:

Top Publications Citing Use of Products

    PCI-32765 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 Idelalisib induced caspase-3 and PARP cleavage at 6 h. Caspase-3 and PAPR cleavage following Ibrutinib (IB), Idelalisib (ID), ABT-199 (ABT), in the presence of absence of CXCL12 (SDF) and AMD3100 (AMD).

    PCI-32765 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.

    PCI-32765 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.

    PCI-32765 purchased from MCE. Usage Cited in: Patent. US 20160222465 A1.

    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. plenti-GFP vector, CXCR4WT and CXCR4S338X expressing BCWM.1 cells are pretreated for 2 hours with either Ibrutinib (0.5 uM) or AMD3100 (30 uM) prior to stimulation with SDF-1a (20 nM) for 2 minutes. Results depict differences in phospho-AKT, phospho-ERK, and phospho-BTK obtained by immunoblotting follow

    PCI-32765 purchased from MCE. Usage Cited in: Patent. US 20160222465 A1.

    CXCR4S338X expressing BCWM.1 and MWCL-1 cells show variable resistance to PARP and caspase 3 cleavage mediated by WM relevant therapeutics in the presence of SDF-1a, and reversed by AMD3100. plenti-GFP vector, CXCR4WT and CXCR4S338X expressing WM cells are treated for 6 hours with Bendamustine (BENDA), Fludarabine (FLUDARA), Bortezomib (BORT), and Idelalisib (IDELA) at their EC50 doses in the presence or absence of SDF-1a (20 nM) and/or the CXCR4 recep

    PCI-32765 purchased from MCE. Usage Cited in: Blood. 2016 Jun 23;127(25):3237-52.

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

    PCI-32765 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
    • Biological Activity

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    • Technical Information

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    Description

    PCI-32765 is a selective, irreversible Btk inhibitor with IC50 value of 0.5 nM.

    IC50 & Target

    IC50: 0.5 nM (Btk)

    In Vitro

    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]. PCI-32765 inhibits BCR-activated primary B cell proliferation (IC50=8 nM). Following FcγR stimulation, PCI-32765 inhibits TNFα, IL-1β and IL-6 production in primary monocytes (IC50=2.6, 0.5, 3.9 nM, respectively)[3].

    In Vivo

    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. PCI-32765 inhibits autoantibody production and the development of kidney disease in the MRL-Fas(lpr) lupus model. PCI-32765 (3.125-50 mg/kg, p.o.) reduces renal disease and autoantibody production in MRL-Fas(lpr) mice[1]. 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]. PCI-32765 dose-dependently and potently reverses arthritic inflammation in a therapeutic CIA model with an ED50 of 2.6 mg/kg/day. PCI-32765 also prevents clinical arthritis in CAIA models[3].

    Clinical Trial
    NCT Number Sponsor Condition Start Date Phase
    NCT02955628 Singapore General Hospital|Janssen, LP Diffuse Large B Cell Lymphoma|Diffuse Large B-Cell Lymphoma Recurrent December 13, 2016 Phase 2
    NCT02801578 M.D. Anderson Cancer Center Chronic Lymphocytic Leukemia July 6, 2016
    NCT02757040 Peking University People's Hospital|Beijing Hospital Leukemia, Lymphocytic, Chronic, B-Cell December 2016 Phase 3
    NCT02973399 Esanex Inc. Cancer February 7, 2017 Phase 1
    NCT02912754 Sunnybrook Health Sciences Centre|Novartis Leukemia, Lymphocytic, Chronic, B-Cell March 2017 Phase 1|Phase 2
    NCT02884453 Royal Marsden NHS Foundation Trust|Janssen, LP Gastrooesophageal Cancer July 2016 Phase 2
    NCT01674322 Janssen Research & Development, LLC Healthy Participants August 2012 Phase 1
    NCT02914327 Esanex Inc. Cancer February 2, 2017 Phase 1
    NCT01833039 Janssen Biotech, Inc.|Pharmacyclics LLC. Relapsed or Refractory Mantle Cell Lymphoma May 15, 2013 Phase 4
    NCT02013128 TG Therapeutics, Inc. Chronic Lymphocytic Leukemia|Mantle Cell Lymphoma December 2013 Phase 1|Phase 2
    NCT02169180 Janssen Pharmaceutical K.K. Lymphoma, Mantle-cell August 2014 Phase 2
    NCT02943473 Icahn School of Medicine at Mount Sinai|Pharmacyclics LLC. High Risk Smoldering Multiple Myeloma November 2016 Phase 2
    NCT02315326 Memorial Sloan Kettering Cancer Center|Pharmacyclics LLC.|Janssen Biotech, Inc. Refractory/Recurrent Primary Central Nervous System Lymphoma (PCNSL)|Refractory/Recurrent Secondary Central Nervous System Lymphoma (SCNSL) December 2014 Phase 1|Phase 2
    NCT02321540 M.D. Anderson Cancer Center|Pharmacyclics LLC.|National Cancer Institute (NCI) Lung Cancer March 31, 2015 Phase 1|Phase 2
    NCT03129828 Prof. Dr. Clemens Schmitt|Charite University, Berlin, Germany|Janssen-Cilag Ltd. Diffuse Large B Cell Lymphoma March 17, 2017 Phase 1|Phase 2
    NCT02558816 Nantes University Hospital|Janssen, LP|Roche Pharma AG Mantle Cell Lymphoma October 14, 2015 Phase 1|Phase 2
    NCT02556892 Janssen Pharmaceutical K.K. Lymphocytic Leukemia July 3, 2015 Phase 1
    NCT02269085 M.D. Anderson Cancer Center|Pharmacyclics LLC.|Amgen Lymphoma April 2015 Phase 1|Phase 2
    NCT02575300 H. Lee Moffitt Cancer Center and Research Institute|Pharmacyclics LLC. Carcinoid Tumors|Pancreatic NET October 9, 2015 Phase 2
    NCT02309580 Memorial Sloan Kettering Cancer Center|Ohio State University|Pharmacyclics LLC.|Janssen Biotech, Inc. T-cell Lymphoma|Relapsed and Refractory T-cell Lymphoma January 2015 Phase 1
    NCT02420912 M.D. Anderson Cancer Center|Bristol-Myers Squibb Leukemia|Chronic Lymphocytic Leukemia June 2015 Phase 2
    NCT02604511 Dana-Farber Cancer Institute|Pharmacyclics LLC. Waldenstrom's Macroglobulinemia January 2016 Phase 2
    NCT02950038 M.D. Anderson Cancer Center|Janssen Scientific Affairs, LLC Lung Cancer, Nonsmall Cell, Stage I December 2016 Phase 2
    NCT02315768 University of California, San Diego|Pharmacyclics LLC. Chronic Lymphocytic Leukemia November 2015 Phase 1|Phase 2
    NCT02272686 M.D. Anderson Cancer Center|Pharmacyclics LLC. Lymphoma June 3, 2016 Phase 2
    NCT01626651 Janssen Research & Development, LLC Healthy June 2012 Phase 1
    NCT02638116 Janssen Research & Development, LLC Healthy January 2016 Phase 1
    NCT02301156 TG Therapeutics, Inc. Chronic Lymphocytic Leukemia January 2015 Phase 3
    NCT02356458 Swiss Group for Clinical Cancer Research Mantle Cell Lymphoma August 2015 Phase 1|Phase 2
    NCT02635074 Bruno C. Medeiros|National Cancer Institute (NCI)|Stanford University Recurrent Adult Acute Myeloid Leukemia November 2016 Phase 1
    NCT02451111 Swiss Group for Clinical Cancer Research|Nordic Lymphoma Group Follicular Lymphoma October 2015 Phase 2
    NCT02682641 Grupo Español de Linfomas y Transplante Autólogo de Médula Ósea|Janssen-Cilag, S.A. Mantle Cell Lymphoma May 2016 Phase 2
    NCT02403271 Pharmacyclics LLC. Non-Small Cell Lung Cancer March 2015 Phase 1|Phase 2
    NCT02388048 Gruppo Italiano Malattie EMatologiche dell'Adulto Leukemia, Lymphoblastic, Chronic October 2015 Phase 2
    NCT02109224 National Cancer Institute (NCI) Adult B Acute Lymphoblastic Leukemia|Chronic Lymphocytic Leukemia|Cutaneous B-Cell Non-Hodgkin Lymphoma|Extranodal Marginal Zone Lymphoma of Mucosa-Associated Lymphoid Tissue|HIV Infection|Intraocular Lymphoma|Multicentric Angiofollicular Lymphoid Hyperplasia|Nodal Marginal Zone Lymphoma|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Burkitt Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Diffuse Small Cleaved Cell Ly September 2014 Phase 1
    NCT01779791 Janssen Research & Development, LLC|Pharmacyclics LLC. Lymphoma April 2013 Phase 2
    NCT02959944 Pharmacyclics LLC.|Janssen Research & Development, LLC Chronic Graft Versus Host Disease December 2016 Phase 3
    NCT02553941 University of California, Davis|Pharmacyclics LLC. Chronic Myelomonocytic Leukemia|de Novo Myelodysplastic Syndrome|Previously Treated Myelodysplastic Syndrome|Refractory Anemia With Excess Blasts in Transformation|Secondary Myelodysplastic Syndrome April 2016 Phase 1
    NCT02670317 Fondazione Italiana Linfomi ONLUS Lymphoma, B-Cell September 2016 Phase 2
    NCT02827617 Oncology Institute of Southern Switzerland Chronic Lymphocytic Leukemia June 2016
    NCT02877225 Janssen Research & Development, LLC Healthy August 29, 2016 Phase 1
    NCT02351037 Pharmacyclics LLC. Acute Myeloid Leukemia (AML) February 2015 Phase 2
    NCT01325701 Pharmacyclics LLC. Diffuse Large Cell B-lymphoma May 2011 Phase 2
    NCT02200848 Georgetown University|National Cancer Institute (NCI) Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma April 2014 Phase 1
    NCT01599949 Janssen Research & Development, LLC|Pharmacyclics LLC. Mantle Cell Lymphoma August 2012 Phase 2
    NCT02381080 Janssen Research & Development, LLC B-Cell Chronic Lymphocytic Leukemia May 2015 Phase 1
    NCT02991638 The University of Hong Kong|Janssen, LP Chronic Lymphocytic Leukemia|Indolent B-cell Lymphomas|Chronic Hepatitis B|Lymphoma, Small Lymphocytic|Mantle-Cell Lymphoma|Waldenstrom's Macroglobulinaemia|Follicular Lymphoma December 2016 Phase 3
    NCT02756897 M.D. Anderson Cancer Center|AbbVie Leukemia|Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma July 7, 2016 Phase 2
    NCT02689869 Ludwig-Maximilians - University of Munich|Hoffmann-La Roche|Janssen-Cilag G.m.b.H Indolent Non-Hodgkin Lymphoma April 2016 Phase 2
    NCT02207062 University of Washington|National Cancer Institute (NCI) Recurrent B-Cell Non-Hodgkin Lymphoma|Recurrent Indolent Adult Non-Hodgkin Lymphoma|Refractory B-Cell Non-Hodgkin Lymphoma October 2014
    NCT01880567 M.D. Anderson Cancer Center|Pharmacyclics LLC.|Janssen Pharmaceuticals Lymphoma July 2013 Phase 2
    NCT02863718 German CLL Study Group Chronic Lymphocytic Leukemia April 2014 Phase 3
    NCT02007044 M.D. Anderson Cancer Center|Pharmacyclics LLC. Leukemia December 2013 Phase 2
    NCT02055924 The Lymphoma Academic Research Organisation|Janssen Pharmaceutica N.V., Belgium B-cell Lymphoma May 2014 Phase 1
    NCT02841150 Janssen Research & Development, LLC Healthy June 2016 Phase 1
    NCT02129062 National Cancer Institute (NCI)|M.D. Anderson Cancer Center Adult B Acute Lymphoblastic Leukemia|Adult B Acute Lymphoblastic Leukemia With t(9;22)(q34;q11.2); BCR-ABL1|Recurrent Adult Acute Lymphoblastic Leukemia April 2014 Phase 2
    NCT03093831 National Cancer Centre, Singapore|Singapore General Hospital|Samsung Medical Center Lymphoma, B-Cell, Marginal Zone July 8, 2016 Phase 2
    NCT02537613 Dana-Farber Cancer Institute|Genentech, Inc. Chronic Lymphocytic Leukemia December 2015 Phase 1
    NCT03130348 Mayo Clinic|National Cancer Institute (NCI) Amyloidosis|Immunoglobulin Light Chain Deposition July 15, 2017 Phase 2
    NCT02436668 Pharmacyclics LLC. Metastatic Pancreatic Adenocarcinoma May 2015 Phase 2|Phase 3
    NCT02626884 University of Cologne Nodular Lymphocyte-Predominant Hodgkin's Lymphoma August 2016 Phase 2
    NCT02159755 National Cancer Institute (NCI) Recurrent Mantle Cell Lymphoma May 2014 Phase 1
    NCT01804686 Janssen Research & Development, LLC|Pharmacyclics LLC. Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma|Mantle Cell Lymphoma|Follicular Lymphoma|Diffuse Large B-cell Lymphoma September 9, 2013 Phase 3
    NCT01589302 Kami Maddocks|Ohio State University Comprehensive Cancer Center Prolymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory/Relapsed Chronic Lymphocytic Leukemia May 21, 2012 Phase 2
    NCT01886859 National Cancer Institute (NCI) B-Cell Prolymphocytic Leukemia|Recurrent Chronic Lymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Small Lymphocytic Lymphoma April 26, 2013 Phase 1
    NCT02966730 Memorial Sloan Kettering Cancer Center|Fox Chase Cancer Center|Pharmacyclics LLC. Follicular Lymphoma|Follicular Lymphoma, Grade 1|Follicular Lymphoma, Grade 2|Follicular Lymphoma Grade IIIa November 2016
    NCT03128879 M.D. Anderson Cancer Center|AbbVie Primary Lymphoid Haematopoietic Neoplasms|Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma June 16, 2017 Phase 2
    NCT01849263 National Cancer Institute (NCI) Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Refractory Follicular Lymphoma April 2013 Phase 2
    NCT02899078 University of California, Davis|Pharmacyclics LLC. Metastatic Renal Cell Cancer|Stage IV Renal Cell Cancer November 2016 Phase 1|Phase 2
    NCT02419560 Craig Portell, MD|AbbVie|University of Virginia Lymphoma, Mantle-Cell|Recurrent Lymphoma, Mantle-Cell April 2015 Phase 1
    NCT02677948 University of Michigan Cancer Center Chronic Lymphocytic Leukemia|Lymphoma, Small Lymphocytic October 2016 Phase 1|Phase 2
    NCT02902965 Pharmacyclics LLC.|Janssen Research & Development, LLC Multiple Myeloma September 2016 Phase 2
    NCT02649387 Mayo Clinic|National Cancer Institute (NCI) Stage I Chronic Lymphocytic Leukemia|Stage II Chronic Lymphocytic Leukemia|Stage III Chronic Lymphocytic Leukemia|Stage IV Chronic Lymphocytic Leukemia February 2016 Phase 2
    NCT02427620 M.D. Anderson Cancer Center|Pharmacyclics LLC. Lymphoma June 2015 Phase 2
    NCT02242097 Northwestern University|Janssen Scientific Affairs, LLC|National Cancer Institute (NCI) Contiguous Stage II Mantle Cell Lymphoma|Noncontiguous Stage II Mantle Cell Lymphoma|Stage I Mantle Cell Lymphoma|Stage III Mantle Cell Lymphoma|Stage IV Mantle Cell Lymphoma January 2015 Phase 2
    NCT02219737 National Cancer Institute (NCI) CD20 Positive|Recurrent Diffuse Large B-Cell Lymphoma|Refractory Diffuse Large B-Cell Lymphoma September 12, 2014 Phase 1
    NCT03149315 Ann & Robert H Lurie Children's Hospital of Chicago|Feinberg School of Medicine, Northwestern University Food Allergy|Anaphylaxis Food April 10, 2017 Phase 2
    NCT02662296 Fred Hutchinson Cancer Research Center|National Cancer Institute (NCI) Prolymphocytic Leukemia|Recurrent Chronic Lymphocytic Leukemia|Recurrent Non-Hodgkin Lymphoma|Recurrent Small Lymphocytic Lymphoma March 2016 Phase 2
    NCT02542514 The Lymphoma Academic Research Organisation Primary Central Nervous Lymphoma|Intraocular Lymphoma September 2015 Phase 2
    NCT02997761 University of California, Davis|National Cancer Institute (NCI)|Pharmacyclics LLC. Adult B Acute Lymphoblastic Leukemia|Philadelphia Chromosome Positive June 2017 Phase 2
    NCT02614508 Emory University|Novartis Recurrent Chronic Lymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Small Lymphocytic Lymphoma January 2016 Phase 1
    NCT01841723 National Cancer Institute (NCI) Hairy Cell Leukemia|Hairy Cell Leukemia Variant April 1, 2013 Phase 2
    NCT02824029 Barbara Ann Karmanos Cancer Institute|National Cancer Institute (NCI) Classical Hodgkin Lymphoma|Recurrent Hodgkin Lymphoma|Refractory Hodgkin Lymphoma June 2016 Phase 2
    NCT02756247 Memorial Sloan Kettering Cancer Center|Janssen Scientific Affairs, LLC|Novartis Pharmaceuticals Lymphoma|Mantle Cell Lymphoma|Follicular Lymphoma|Diffuse Large B Cell Lymphoma May 2016 Phase 1
    NCT01980654 Pharmacyclics LLC. Follicular Lymphoma|B-cell Lymphoma|Non-Hodgkin's Lymphoma December 2013 Phase 2
    NCT02611908 Michael Choi|Pharmacyclics LLC.|University of California, San Diego Chronic Lymphocytic Leukemia June 2016 Phase 1
    NCT02160015 National Cancer Institute (NCI) Recurrent Chronic Lymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Small Lymphocytic Lymphoma|Stage III Chronic Lymphocytic Leukemia|Stage III Small Lymphocytic Lymphoma|Stage IV Chronic Lymphocytic Leukemia|Stage IV Small Lymphocytic Lymphoma May 9, 2014 Phase 1
    NCT01744691 Pharmacyclics LLC.|Janssen Research & Development, LLC Chronic Lymphocytic Leukemia With 17p Deletion|Small Lymphocytic Lymphoma With 17p Deletion January 2013 Phase 2
    NCT03190330 Johnson & Johnson Private Limited Leukemia, Lymphocytic, Chronic, B-Cell July 5, 2017 Phase 4
    NCT02514083 National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) CLL (Chronic Lymphocytic Leukemia)|SLL (Small Lymphocytic Lymphoma) July 28, 2015 Phase 2
    NCT03198026 Sidney Kimmel Cancer Center at Thomas Jefferson University|Genentech, Inc.|Pharmacyclics LLC.|Thomas Jefferson University Non-Hodgkin's Lymphoma November 2017 Phase 2
    NCT02562898 Margaret Tempero|University of California, San Francisco Metastatic Pancreatic Adenocarcinoma October 2015 Phase 1|Phase 2
    NCT01829568 National Cancer Institute (NCI)|Celgene Corporation CD20 Positive|Stage II Grade 1 Contiguous Follicular Lymphoma|Stage II Grade 1 Non-Contiguous Follicular Lymphoma|Stage II Grade 2 Contiguous Follicular Lymphoma|Stage II Grade 2 Non-Contiguous Follicular Lymphoma|Stage II Grade 3 Contiguous Follicular Lymphoma|Stage II Grade 3 Non-Contiguous Follicular Lymphoma|Stage III Grade 1 Follicular Lymphoma|Stage III Grade 2 Follicular Lymphoma|Stage III Grade 3 Follicular Lymphoma|Stage IV Grade 1 Follicular Lymphoma|Stage IV Grade 2 Follicular Lymphom June 21, 2013 Phase 1
    NCT02940301 Ohio State University Comprehensive Cancer Center|National Cancer Institute (NCI) Classical Hodgkin Lymphoma December 20, 2016 Phase 2
    NCT03053440 BeiGene Waldenström's Macroglobulinemia January 25, 2017 Phase 3
    NCT02581930 Duke University|National Cancer Institute (NCI) Metastatic Melanoma|Recurrent Melanoma of the Skin|Stage IV Skin Melanoma August 2016 Phase 2
    NCT02232386 Gruppo Italiano Malattie EMatologiche dell'Adulto Chronic Lymphocyte Leukemia|Adult Patients February 2015 Phase 2
    NCT02815059 University of Utah|Janssen, LP Acute Lymphoblastic Leukemia September 2016 Phase 1
    NCT02195869 Pharmacyclics LLC. Graft Versus Host Disease July 2014 Phase 1|Phase 2
    NCT02636322 M.D. Anderson Cancer Center|Celgene|Janssen Scientific Affairs, LLC Lymphoma March 2016 Phase 2
    NCT02532257 M.D. Anderson Cancer Center|Janssen, LP Lymphoma|Follicular Lymphoma (FL) April 2016 Phase 2
    NCT02736617 OHSU Knight Cancer Institute|Genentech, Inc.|National Cancer Institute (NCI) Recurrent Mantle Cell Lymphoma|Refractory Mantle Cell Lymphoma May 2016 Phase 2
    NCT02869633 Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI) Blastoid Variant Mantle Cell Lymphoma|Recurrent Chronic Lymphocytic Leukemia|Recurrent Follicular Lymphoma|Recurrent Hodgkin Lymphoma|Recurrent Mantle Cell Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Follicular Lymphoma|Refractory Hodgkin Lymphoma|Refractory Mantle Cell Lymphoma September 2016 Phase 2
    NCT03021460 Mayo Clinic|National Cancer Institute (NCI) Metastatic Melanoma|Stage III Skin Melanoma|Stage IIIA Skin Melanoma|Stage IIIB Skin Melanoma|Stage IIIC Skin Melanoma|Stage IV Skin Melanoma January 31, 2017 Phase 2
    NCT02744612 City of Hope Medical Center|National Cancer Institute (NCI)|Pharmacyclics LLC. Recurrent Hodgkin Lymphoma|Refractory Hodgkin Lymphoma June 2016 Phase 2
    NCT03088878 University of California, San Diego B-cell Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma|Mantle Cell Lymphoma August 1, 2017 Phase 1|Phase 2
    NCT02415608 Jason Robert Gotlib|National Cancer Institute (NCI)|Stanford University Aggressive Systemic Mastocytosis|Mast Cell Leukemia|Systemic Mastocytosis March 2015 Phase 2
    NCT02947347 Pharmacyclics LLC. Treatment Naive Follicular Lymphoma January 2017 Phase 3
    NCT01722487 Pharmacyclics LLC.|Janssen Research & Development, LLC Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma March 2013 Phase 3
    NCT02329847 Janssen Research & Development, LLC|Bristol-Myers Squibb Hematologic Neoplasms March 11, 2015 Phase 1|Phase 2
    NCT02582320 Gruppo Italiano Malattie EMatologiche dell'Adulto Chronic Lymphocytic Leukemia March 2016
    NCT03045328 Steven E. Coutre|Stanford University Recurrent Chronic Lymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Small Lymphocytic Lymphoma March 2017 Phase 1|Phase 2
    NCT02703272 Janssen Research & Development, LLC Lymphoma, Non-Hodgkin July 1, 2016 Phase 3
    NCT02874404 Matthew Lunning, MD|National Cancer Institute (NCI)|University of Nebraska Recurrent Diffuse Large B-Cell Lymphoma|Refractory Diffuse Large B-Cell Lymphoma June 16, 2016 Phase 2
    NCT02345863 German CLL Study Group Chronic Lymphocytic Leucemia January 2015 Phase 2
    NCT01646021 Janssen Research & Development, LLC|Pharmacyclics LLC. Mantle Cell Lymphoma December 2012 Phase 3
    NCT02165397 Pharmacyclics LLC.|Janssen Research & Development, LLC Waldenström's Macroglobulinemia July 2014 Phase 3
    NCT02006485 TG Therapeutics, Inc. Chronic Lymphocytic Leukemia|Non-Hodgkin's Lymphoma December 2013 Phase 1
    NCT03136497 Hackensack University Medical Center|Janssen Scientific Affairs, LLC|Genentech, Inc. Relapsed Diffuse Large B-Cell Lymphoma|Refractory Diffuse Large B-Cell Lymphoma May 30, 2017 Phase 1
    NCT01955499 National Cancer Institute (NCI) Recurrent Diffuse Large B-Cell Lymphoma|Recurrent Follicular Lymphoma|Recurrent Lymphoplasmacytic Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Refractory Diffuse Large B-Cell Lymphoma|Refractory Follicular Lymphoma|Refractory Lymphoplasmacytic Lymphoma|Refractory Mantle Cell Lymphoma September 13, 2013 Phase 1
    NCT02427451 Jeffrey Jones|Ohio State University Comprehensive Cancer Center Chronic Lymphocytic Leukemia|Refractory Chronic Lymphocytic Leukemia July 2015 Phase 1|Phase 2
    NCT02758665 University of Ulm|German CLL Study Group|Roche Pharma AG|Janssen-Cilag Ltd. Leukemia, Lymphocytic, Chronic September 2016 Phase 2
    NCT01578707 Pharmacyclics LLC.|Janssen Research & Development, LLC Relapsed or Refractory Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma June 2012 Phase 3
    NCT02251548 Dana-Farber Cancer Institute|Pharmacyclics LLC. Chronic Lymphocytic Leukemia|Leukemia October 2014 Phase 2
    NCT02437019 Janssen-Cilag Farmaceutica Ltda. B-cell Chronic Lymphocytic Leukemia
    NCT02689141 German CLL Study Group Chronic Lymphocytic Leukemia January 2016 Phase 2
    NCT02956382 Georgetown University|AbbVie|Pharmacyclics LLC.|Hackensack University Medical Center Refractory Follicular Lymphoma|Relapsed Follicular Lymphoma November 2016 Phase 1|Phase 2
    NCT02477696 Acerta Pharma BV Chronic Lymphocytic Leukemia June 2015 Phase 3
    NCT02759016 Boehringer Ingelheim Leukemia, Lymphocytic, Chronic, B-Cell June 23, 2016 Phase 1
    NCT02743546 Janssen Research & Development, LLC Leukemia, Lymphocytic, Chronic, B-Cell|Lymphoma, Large B-Cell, Diffuse|Lymphoma, Follicular|Lymphoma, Mantle-Cell August 2016 Phase 1
    NCT02927964 Robert Lowsky|National Cancer Institute (NCI)|Stanford University Grade 1 Follicular Lymphoma|Grade 2 Follicular Lymphoma|Grade 3a Follicular Lymphoma|Recurrent Follicular Lymphoma|Refractory Follicular Lymphoma November 2016 Phase 1|Phase 2
    NCT02271438 Janssen Research & Development, LLC Healthy October 2014 Phase 1
    NCT02303392 Jennifer Woyach|National Cancer Institute (NCI)|Karyopharm Therapeutics Inc|Ohio State University Comprehensive Cancer Center Prolymphocytic Leukemia|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia March 11, 2015 Phase 1
    NCT02910583 Pharmacyclics LLC.|Janssen Research & Development, LLC Leukemia, Chronic Lymphocytic|Lymphoma, Small Lymphocytic October 2016 Phase 2
    NCT01611090 Janssen Research & Development, LLC|Pharmacyclics LLC. Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma September 19, 2012 Phase 3
    NCT02268851 Dana-Farber Cancer Institute|TG Therapeutics, Inc.|The Leukemia and Lymphoma Society Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma|Mantle Cell Lymphoma November 2014 Phase 1
    NCT03153202 Joshua Brody|Merck Sharp & Dohme Corp.|Icahn School of Medicine at Mount Sinai Chronic Lymphocytic Leukemia|Mantle Cell Lymphoma May 2017 Phase 1|Phase 2
    NCT02643667 Lawrence Fong|University of California, San Francisco Prostate Cancer December 2016 Phase 1|Phase 2
    NCT02471391 Peter MacCallum Cancer Centre, Australia Mantle Cell Lymphoma June 2015 Phase 2
    NCT02629809 M.D. Anderson Cancer Center|Genentech, Inc.|Pharmacyclics LLC. Leukemia|Chronic Lymphocytic Leukemia March 2016 Phase 2
    NCT02692248 Grupo Español de Linfomas y Transplante Autólogo de Médula Ósea|Janssen-Cilag, S.A. Diffuse Large B-Cell Lymphoma April 2016 Phase 2
    NCT03145480 Northwell Health|Pharmacyclics LLC. Richter Syndrome July 2017 Phase 2
    NCT02599324 Pharmacyclics LLC. Renal Cell Carcinoma (RCC)|Urothelial Carcinoma|Gastric Adenocarcinoma|Colorectal Adenocarcinoma (CRC) November 2015 Phase 1|Phase 2
    NCT02203526 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Primary Central Nervious System Lymphoma July 24, 2014 Phase 1
    NCT03015792 Mayo Clinic|National Cancer Institute (NCI) Recurrent Plasma Cell Myeloma|Refractory Plasma Cell Myeloma March 10, 2017 Phase 1|Phase 2
    NCT03112174 Pharmacyclics LLC.|Janssen Research & Development, LLC Mantle-Cell Lymphoma April 2017 Phase 3
    NCT02390609 Janssen Research & Development, LLC Healthy March 2015 Phase 1
    NCT02760485 Incyte Corporation Diffuse Large B-cell Lymphoma December 2016 Phase 1|Phase 2
    NCT02780830 AstraZeneca Core: Relapsed or Refractory Diffuse Large B-Cell Lymphoma|Module 1: Non-GCB Diffuse Large B-Cell Lymphoma June 2016 Phase 1
    NCT02548962 Pharmacyclics LLC.|Celgene Corporation Multiple Myeloma March 2016 Phase 1|Phase 2
    NCT02518555 Farrukh Awan|Pharmacyclics LLC.|Ohio State University Comprehensive Cancer Center Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma December 2015 Phase 2
    NCT02077166 Pharmacyclics LLC.|Janssen Research & Development, LLC|Celgene Corporation Relapsed Diffuse Large B-Cell Lymphoma|Refractory Diffuse Large B-Cell Lymphoma February 2014 Phase 1|Phase 2
    NCT02460276 Lund University Hospital|Celgene|Janssen, LP|Nordic Lymphoma Group Relapsed/Refractory Mantle Cell Lymphoma April 2015 Phase 2
    NCT01973387 Janssen Research & Development, LLC|Pharmacyclics LLC. Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma October 28, 2013 Phase 3
    NCT01855750 Janssen Research & Development, LLC|Pharmacyclics LLC. Lymphoma September 3, 2013 Phase 3
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    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) 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
    Cell Assay
    [3]

    PCI-32765 is dissolved in DMSO.

    Primary human B cells are isolated from peripheral blood mononuclear cell of healthy human volunteers by Ficoll-Hypaque gradient separation followed by negative selection using human Miltenyl human B cell Isolation Kit II. In 0.2 mL RPMI plus 10% FBS, 100,000 B cells are treated with 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.

    Animal Administration
    [3]

    CI-32765 is formulated in 1% methylcellulose, 0.4% Cremephor® EL, and 98.09% water.

    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). 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.

    References
    M.Wt

    440.5

    Formula

    C₂₅H₂₄N₆O₂

    CAS No.

    936563-96-1

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 52 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.87% ee.: 99.50%

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    Product Name:
    PCI-32765
    Cat. No.:
    HY-10997
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