1. Protein Tyrosine Kinase/RTK
    Autophagy
  2. Bcr-Abl
    Src
    Autophagy

Dasatinib (Synonyms: BMS-354825)

Cat. No.: HY-10181 Purity: 99.84%
Data Sheet SDS Handling Instructions

Dasatinib is a potent and dual AblWT/Src inhibitor IC50 of 0.6 nM/0.8 nM respectively; also inhibits c-KitWT/c-KitD816V with IC50 of 79 nM/37 nM.

For research use only. We do not sell to patients.
Dasatinib Chemical Structure

Dasatinib Chemical Structure

CAS No. : 302962-49-8

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Other Forms of Dasatinib:

    Dasatinib purchased from MCE. Usage Cited in: Leukemia. 2012 Oct;26(10):2233-44.

    Drug combination effect on phosphorylation of AKT. Expression of phospho-AKT and total AKT in MOLM13 cells treated for 15 minutes with DMSO vehicle, PKC412 (2.5 nM), Dasatinib (165 nM), or a combination of both. Protein lysates are prepared from MOLM13 cells, and are analyzed via immunoblotting with antibodies to phospho-AKT and total AKT.

    Dasatinib purchased from MCE. Usage Cited in: Leukemia. 2012 Oct;26(10):2233-44.

    SCM stimulation of phospho-STAT5 and drug combination effect on phosphorylation of phospho-STAT5. Expression of phospho-STAT5 and total STAT5 in MOLM13 cells treated for 1.5 h with DMSO vehicle, PKC412 (5 nM), KIN40 (82.5 nM) or a combination of both. Results shown are representative of two independent experiments in which similar results are observed.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Dasatinib is a potent and dual AblWT/Src inhibitor IC50 of 0.6 nM/0.8 nM respectively; also inhibits c-KitWT/c-KitD816V with IC50 of 79 nM/37 nM.

    IC50 & Target

    IC50: 0.6 nM/0.8 nM (AblWT/Src)[1]
    IC50: 79 nM/37 nM (c-KitWT/c-KitD816V)[2]

    In Vitro

    Dasatinib potently inhibits wild-type Abl kinase and all mutants except T315I over a narrow range (IC50≤1.7 nM). Dasatinib (IC50: 0.8 nM) displays 325-fold greater potency compared with Imatinib against cells expressing wild-type Bcr-Abl in Ba/F3 cells[1].

    In Vivo

    Daily treatment with Dasatinib (50 mg/kg) is initiated on day 10. Using this approach, a significant inhibition of BCPAP orthotopic tumor growth is observed 6 days after treatment (day 16, P=0.014), which is sustained through days 23 and 29 (P=0.0003), compared with vehicle-treated mice[3]. Metabolism studies of Dasatinib (50 mg/kg) in rat suggested that Dasatinib is the major circulating component, whereas multiple metabolites contributed to the remaining 40-60% of the sample radioactivity at 4 h post dose[4].

    Clinical Trial
    NCT Number Sponsor Condition Start Date Phase
    NCT00364286 M.D. Anderson Cancer Center|Bristol-Myers Squibb Leukemia|Lymphoma August 2006 Phase 2
    NCT00254423 M.D. Anderson Cancer Center|Bristol-Myers Squibb Chronic Myelogenous Leukemia November 2005 Phase 2
    NCT00255346 M.D. Anderson Cancer Center|Bristol-Myers Squibb Acute Myeloid Leukemia|Myelodysplastic Syndromes|Agnogenic Myeloid Metaplasia|Myelofibrosis|Hypereosinophilic Syndrome|Polycythemia Vera|Mastocytosis|Leukemia, Myelomonocytic, Chronic November 15, 2005 Phase 2
    NCT00388427 University of Pittsburgh|Bristol-Myers Squibb Malignant Solid Tumour June 2007 Phase 1
    NCT00364286 M.D. Anderson Cancer Center|Bristol-Myers Squibb Leukemia|Lymphoma August 2006 Phase 2
    NCT00254423 M.D. Anderson Cancer Center|Bristol-Myers Squibb Chronic Myelogenous Leukemia November 2005 Phase 2
    NCT00255346 M.D. Anderson Cancer Center|Bristol-Myers Squibb Acute Myeloid Leukemia|Myelodysplastic Syndromes|Agnogenic Myeloid Metaplasia|Myelofibrosis|Hypereosinophilic Syndrome|Polycythemia Vera|Mastocytosis|Leukemia, Myelomonocytic, Chronic November 15, 2005 Phase 2
    NCT00388427 University of Pittsburgh|Bristol-Myers Squibb Malignant Solid Tumour June 2007 Phase 1
    NCT00895297 European Group for Blood and Marrow Transplantation|Bristol-Myers Squibb Chronic Myeloid Leukemia February 2010 Phase 2
    NCT03216070 Hospital Universitario Dr. Jose E. Gonzalez Chronic Myelogenous Leukemia April 1, 2016 Phase 4
    NCT01310010 Grupo Espanol de trasplantes hematopoyeticos y terapia celular Leukemia, Lymphoblastic, Acute, Philadelphia-Positive April 2010 Phase 2
    NCT01643603 Barbara Ann Karmanos Cancer Institute|National Cancer Institute (NCI) Non-Hodgkin's Lymphoma|Hodgkin's Lymphoma|Myeloid Leukemia|Multiple Myeloma|Myelodysplastic Syndrome|Lymphoid Leukemia May 2012 Phase 1|Phase 2
    NCT00882583 Sidney Kimmel Comprehensive Cancer Center|Bristol-Myers Squibb Head and Neck Cancer July 2009 Phase 1|Phase 2
    NCT03193281 University of Auckland, New Zealand|Leukaemia & Blood Cancer New Zealand Chronic Myeloid Leukemia July 2017 Phase 2
    NCT01051115 Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA) Chronic Lymphocytic Leukemia October 2008 Phase 2
    NCT01342679 Kanto CML Study Group|Epidemiological and Clinical Research Information Network Chronic Myeloid Leukemia April 2011 Phase 2
    NCT00429949 Washington University School of Medicine Relapsed, Refractory or Plateau Phase Multiple Myeloma January 2007 Phase 2
    NCT01627132 Shimousa Hematology Study Group|Epidemiological and Clinical Research Information Network Chronic Myeloid Leukemia February 2012 Phase 2
    NCT01744652 M.D. Anderson Cancer Center|Pfizer Advanced Cancers March 2013 Phase 1
    NCT00858403 H. Lee Moffitt Cancer Center and Research Institute|Bristol-Myers Squibb Lung Cancer March 2009 Phase 2
    NCT00787267 Duke University|Bristol-Myers Squibb Non Small Cell Lung Cancer September 2008 Phase 2
    NCT01609816 Barbara Ann Karmanos Cancer Institute|National Cancer Institute (NCI) Non-Hodgkin's Lymphoma|Multiple|Mycosis Fungoides|Hodgkin's Lymphoma|Multiple Myeloma May 2012 Phase 1|Phase 2
    NCT01398046 University of California, San Francisco|Genentech, Inc. Healthy August 2011 Phase 1
    NCT00624585 H. Lee Moffitt Cancer Center and Research Institute|Bristol-Myers Squibb Myelodysplastic Syndromes February 2008
    NCT00979160 Federico II University|University of Bologna Systemic Mastocytosis November 2009 Phase 2
    NCT00820170 Memorial Sloan Kettering Cancer Center|Bristol-Myers Squibb Breast Cancer January 2009 Phase 1|Phase 2
    NCT00566618 M.D. Anderson Cancer Center|Bristol-Myers Squibb Breast Cancer|Bone Metastases November 2007 Phase 1|Phase 2
    NCT00564876 Duke University|Bristol-Myers Squibb Carcinoma, Non-Small-Cell Lung November 2007 Phase 2
    NCT02047149 University of Massachusetts, Worcester|Bristol-Myers Squibb Chronic Myelogenous Leukemia January 2014 Phase 1
    NCT00652574 M.D. Anderson Cancer Center|Bristol-Myers Squibb|United States Department of Defense Malignant Pleural Mesothelioma March 2008 Phase 1
    NCT00608361 National Cancer Institute (NCI) Adult Acute Lymphoblastic Leukemia in Remission|Adult B Acute Lymphoblastic Leukemia|Adult Hepatocellular Carcinoma|Adult Nasal Type Extranodal NK/T-Cell Lymphoma|Adult Solid Neoplasm|Adult T Acute Lymphoblastic Leukemia|Advanced Adult Hepatocellular Carcinoma|Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-Cell Lymphoma|Chronic Lymphocytic Leukemia|Cutaneous B-Cell Non-Hodgkin Lymphoma|Extranodal Marginal Zone Lymphoma of Mucosa-Associated Lymphoid Tissue|Hepatosplenic T-Cell Lymphoma|Intra October 2008 Phase 1
    NCT00438854 Massachusetts General Hospital|Brigham and Women's Hospital|Dana-Farber Cancer Institute|Bristol-Myers Squibb Chronic Lymphocytic Leukemia December 2006 Phase 2
    NCT02389309 M.D. Anderson Cancer Center Solid Tumors October 5, 2015 Phase 1
    NCT00597038 H. Lee Moffitt Cancer Center and Research Institute|Bristol-Myers Squibb Metastatic Melanoma November 2007 Phase 1|Phase 2
    NCT00162214 Bristol-Myers Squibb Tumors August 2005 Phase 1
    NCT01660906 Bristol-Myers Squibb Chronic Phase Chronic Myeloid Leukemia December 2012 Phase 4
    NCT00609999 Duke University|Bristol-Myers Squibb|Genentech, Inc. Glioblastoma|Gliosarcoma January 2008 Phase 1
    NCT01491633 Dana-Farber Cancer Institute Squamous Cell Lung Cancer September 2011 Phase 2
    NCT02689440 M.D. Anderson Cancer Center Chronic Myelogenous Leukemia February 2016 Phase 4
    NCT00568750 Swiss Group for Clinical Cancer Research Gastrointestinal Stromal Tumor December 2007 Phase 2
    NCT00672295 AA Secord|Duke University Ovarian Cancer|Peritoneal Cancer|Fallopian Tube Cancer August 2007 Phase 1
    NCT01441882 OHSU Knight Cancer Institute|National Cancer Institute (NCI) Refractory Chronic Lymphocytic Leukemia|Stage I Chronic Lymphocytic Leukemia|Stage II Chronic Lymphocytic Leukemia|Stage III Chronic Lymphocytic Leukemia|Stage IV Chronic Lymphocytic Leukemia October 2011 Phase 2
    NCT02389972 Bristol-Myers Squibb Leukemia, Myelogenous, Chronic, BCR-ABL Positive April 11, 2013
    NCT00459108 National Cancer Institute (NCI) Adult Primary Hepatocellular Carcinoma|Advanced Adult Primary Liver Cancer|Recurrent Adult Primary Liver Cancer April 2007 Phase 2
    NCT00866736 Kanto CML Study Group|Epidemiological and Clinical Research Information Network Chronic Myeloid Leukemia March 2009 Phase 2
    NCT02268370 University Health Network, Toronto|Ozmosis Research Inc. Chronic Myeloid Leukemia October 2014 Phase 2
    NCT01850004 Bristol-Myers Squibb|ICON plc|PPD|Molecular MD|European Organisation for Research and Treatment of Cancer - EORTC|MultiPharma|Steering Committee Chronic Phase Chronic Myeloid Leukemia October 2013 Phase 2
    NCT00470054 National Cancer Institute (NCI) Extensive Stage Small Cell Lung Cancer|Limited Stage Small Cell Lung Cancer|Recurrent Small Cell Lung Cancer April 2007 Phase 2
    NCT00546104 Duke University|Bristol-Myers Squibb Advanced Breast Cancer October 2007 Phase 2
    NCT01015222 M.D. Anderson Cancer Center Advanced Cancer November 2009 Phase 1
    NCT01652976 University of Florida Pancreatic Cancer Metastatic July 2012 Phase 2
    NCT01876212 Walter J. Storkus|National Cancer Institute (NCI)|University of Pittsburgh Metastatic Melanoma November 2013 Phase 2
    NCT01724879 Johann Wolfgang Goethe University Hospital Philadelphia Positive Acute Lymphoblastic Leukemia November 2011 Phase 2
    NCT02129166 University of Florida Healthy Volunteers September 2014 Phase 1
    NCT02297139 Bristol-Myers Squibb Multiple Indications Cancer July 17, 2015 Phase 2
    NCT01218477 Bristol-Myers Squibb Leukemia January 2011 Phase 1|Phase 2
    NCT02428855 Massachusetts General Hospital|Bristol-Myers Squibb|TargetCancer Foundation Cholangiocarcinoma April 2015 Phase 2
    NCT00817531 Baylor Breast Care Center|M.D. Anderson Cancer Center Breast Cancer December 2008 Phase 2
    NCT00570700 University of California, Irvine|Bristol-Myers Squibb Hormone-refractory Prostate Cancer|Adenocarcinoma of the Prostate|Hormone-resistant Prostate Cancer|Prostate Cancer|Recurrent Prostate Cancer July 2007 Phase 2
    NCT01916785 Versailles Hospital|Maisonneuve-Rosemont Hospital|University Hospital, Bordeaux Chronic Myelogenous Leukemia, BCR/ABL Positive May 2009 Phase 2
    NCT00371345 Bristol-Myers Squibb Breast Cancer|Metastasis December 2006 Phase 2
    NCT01426334 National Cancer Institute (NCI) Accelerated Phase Chronic Myelogenous Leukemia|Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Chronic Phase Chronic Myelogenous Leukemia|Relapsing Chronic Myelogenous Leukemia September 2011 Phase 1
    NCT02011945 Bristol-Myers Squibb Chronic Myeloid Leukemia February 7, 2014 Phase 1
    NCT00918463 Weill Medical College of Cornell University|Bristol-Myers Squibb Diffuse Large B-cell Lymphoma June 2009 Phase 2
    NCT00949988 University of California, San Diego|Bristol-Myers Squibb Chronic Lymphocytic Leukemia May 2009 Phase 1|Phase 2
    NCT00924352 Accelerated Community Oncology Research Network|Bristol-Myers Squibb Metastatic Breast Cancer June 2009 Phase 1|Phase 2
    NCT01445509 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Solid Tumors October 27, 2008 Phase 1
    NCT00826449 M.D. Anderson Cancer Center|Bristol-Myers Squibb|OSI Pharmaceuticals Lung Cancer|Non-Small Cell Lung Cancer February 2009 Phase 1|Phase 2
    NCT00852566 Norwegian University of Science and Technology Chronic Myeloid Leukemia March 2009 Phase 2
    NCT01482728 University of Virginia Endometrial Cancer January 2012 Early Phase 1
    NCT00423735 National Cancer Institute (NCI) Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Recurrent Adult Brain Neoplasm January 2007 Phase 2
    NCT01306942 Spanish Breast Cancer Research Group|Bristol-Myers Squibb Breast Cancer July 2011 Phase 1|Phase 2
    NCT00439270 Bristol-Myers Squibb Metastatic Prostate Cancer July 2007 Phase 1|Phase 2
    NCT02059265 National Cancer Institute (NCI) Endometrial Clear Cell Adenocarcinoma|Estrogen Receptor Negative|Ovarian Clear Cell Cystadenocarcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Recurrent Uterine Corpus Carcinoma February 2014 Phase 2
    NCT01802450 PETHEMA Foundation|Dynamic Solutions|Bristol-Myers Squibb Chronic Myeloid Leukemia March 2013 Phase 2
    NCT00563290 National Cancer Institute (NCI) Recurrent Skin Cancer|Squamous Cell Carcinoma of the Skin|Stage 0 Chronic Lymphocytic Leukemia|Stage I Chronic Lymphocytic Leukemia November 2007 Phase 2
    NCT01392703 Bristol-Myers Squibb Pharmacokinetic Study in Healthy Participants July 2011 Phase 1
    NCT00671788 Gynecologic Oncology Group|National Cancer Institute (NCI) Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma June 2008 Phase 2
    NCT01498445 M.D. Anderson Cancer Center|Bristol-Myers Squibb Leukemia June 12, 2012 Phase 1|Phase 2
    NCT03079505 Hamad Medical Corporation Chronic Myeloid Leukemia - Chronic Phase June 2017 Phase 3
    NCT01357655 Bristol-Myers Squibb Leukemia September 2011 Phase 2
    NCT00940524 Memorial Sloan Kettering Cancer Center|Bristol-Myers Squibb Leukemia|Acute Lymphoblastic Leukemia July 2009 Phase 1
    NCT00538980 Weill Medical College of Cornell University|Bristol-Myers Squibb Polycythemia Vera April 30, 2007 Phase 2
    NCT01395017 Otsuka Pharmaceutical Development & Commercialization, Inc. Pancreatic Cancer June 2011 Phase 2
    NCT00429234 M.D. Anderson Cancer Center|Bristol-Myers Squibb Advanced Cancer|Solid Tumors January 2007 Phase 1
    NCT00655746 Bristol-Myers Squibb Healthy April 2008 Phase 1
    NCT00459342 National Cancer Institute (NCI) Non-small Cell Lung Cancer|Recurrent Non-small Cell Lung Cancer|Stage IIIB Non-small Cell Lung Cancer|Stage IV Non-small Cell Lung Cancer March 2007 Phase 2
    NCT00339144 Bristol-Myers Squibb Tumors January 2007 Phase 1
    NCT00436605 National Cancer Institute (NCI) Recurrent Melanoma|Stage IIIA Melanoma|Stage IIIB Melanoma|Stage IIIC Melanoma|Stage IV Melanoma December 2006 Phase 2
    NCT00464620 Sarcoma Alliance for Research through Collaboration|Bristol-Myers Squibb Rhabdomyosarcoma|Malignant Peripheral Nerve Sheath Tumors|Chondrosarcoma|Sarcoma, Ewing's|Sarcoma, Alveolar Soft Part|Chordoma|Epithelioid Sarcoma|Giant Cell Tumor of Bone|Hemangiopericytoma|Gastrointestinal Stromal Tumor (GIST) May 2007 Phase 2
    NCT00892190 University of Pittsburgh Acute Myelogenous Leukemia|Myelodysplastic Syndrome April 2011 Phase 1
    NCT01660971 National Cancer Institute (NCI) Metastatic Pancreatic Adenocarcinoma|Recurrent Pancreatic Carcinoma|Stage III Pancreatic Cancer AJCC v6 and v7|Stage IV Pancreatic Cancer AJCC v6 and v7 July 30, 2012 Phase 1
    NCT00767520 Bristol-Myers Squibb Breast Cancer February 2009 Phase 2
    NCT00717704 Washington Hospital Center|Bristol-Myers Squibb Solid Tumor July 2008 Phase 1
    NCT00474812 National Cancer Institute (NCI) Adenocarcinoma of the Pancreas|Recurrent Pancreatic Cancer|Stage IV Pancreatic Cancer May 2007 Phase 2
    NCT00854841 Pusan National University Hospital Chronic Myeloid Leukemia
    NCT00509041 Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) Malignant Mesothelioma August 2007 Phase 2
    NCT00895128 M.D. Anderson Cancer Center Advanced Cancer April 2009 Phase 1
    NCT00706641 Hoosier Cancer Research Network|Bristol-Myers Squibb Transitional Cell Carcinoma of the Bladder June 2008
    NCT01460693 Newcastle University|Newcastle-upon-Tyne Hospitals NHS Trust|Bristol-Myers Squibb|Institute of Cancer Research, United Kingdom|Hammersmith Hospitals NHS Trust Myeloid Leukemia, Chronic, Chronic Phase August 2008 Phase 3
    NCT01826838 Dr Anthony Mega|Brown University Prostate Cancer January 2013 Phase 1
    NCT02720185 University of Wisconsin, Madison|National Cancer Institute (NCI) Breast Neoplasms|Triple Negative Breast Neoplasms July 2016 Phase 2
    NCT01488318 University of Pittsburgh|Bristol-Myers Squibb Squamous Cell Carcinoma Of The Head And Neck October 2013 Phase 2
    NCT01725204 Norwegian University of Science and Technology Leukemia, Myeloid, Chronic-Phase September 2012 Phase 2
    NCT00507767 National Cancer Institute (NCI) Metastatic Squamous Neck Cancer With Occult Primary Squamous Cell Carcinoma|Recurrent Metastatic Squamous Neck Cancer With Occult Primary|Recurrent Salivary Gland Cancer|Recurrent Squamous Cell Carcinoma of the Hypopharynx|Recurrent Squamous Cell Carcinoma of the Larynx|Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity|Recurrent Squamous Cell Carcinoma of the Nasopharynx|Recurrent Squamous Cell Carcinoma of the Oropharynx|Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Na July 2007 Phase 2
    NCT02776878 Beijing Cancer Hospital Gastrointestinal Stromal Tumor May 2016
    NCT00787852 Brown University|Rhode Island Hospital|Memorial Hospital of Rhode Island Non-Small Cell Lung Cancer March 2009 Phase 1
    NCT01004497 The Catholic University of Korea Acute Lymphoblastic Leukemia March 2010 Phase 2
    NCT01092728 M.D. Anderson Cancer Center|Bristol-Myers Squibb Melanoma March 2011 Phase 2
    NCT00481247 Bristol-Myers Squibb Myeloid Leukemia, Chronic September 2007 Phase 3
    NCT01644773 St. Jude Children's Research Hospital Diffuse Intrinsic Pontine Glioma|High-grade Glioma November 27, 2012 Phase 1
    NCT00306202 Bristol-Myers Squibb|Innovative Therapies For Children with Cancer Consortium Leukemia February 22, 2006 Phase 1
    NCT00850382 University of Ulm Acute Myeloid Leukemia (AML) June 2009 Phase 1|Phase 2
    NCT01460160 Bristol-Myers Squibb|Children's Oncology Group|EsPhALL - European Intergroup Study on Post Induction Treatment of Philadelphia Positive Acute Lymphoblastic Leukaemia with Imatinib Leukemia, Pediatric January 30, 2012 Phase 2
    NCT00996723 St. Jude Children's Research Hospital|AstraZeneca|The Cure Starts Now Foundation|Tyler's Treehouse Diffuse Intrinsic Pontine Glioma October 2009 Phase 1
    NCT02113319 University Hospital, Angers Acute Myelogenous Leukemia April 2007 Phase 2
    NCT01761890 Gruppo Italiano Malattie EMatologiche dell'Adulto Chronic Myeloid Leukemia January 2014
    NCT01514864 Bristol-Myers Squibb Carcinoma, Non-small Cell Lung May 2012 Phase 2
    NCT00570401 Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) Lung Cancer June 2006 Phase 2
    NCT01876953 City of Hope Medical Center|National Cancer Institute (NCI) Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Del(5q)|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(15;17)(q22;q12)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Recurrent Adult Acute Myeloid Leukemia|Secondary Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia September 10, 2013 Phase 1|Phase 2
    NCT00504153 National Cancer Institute (NCI) Recurrent Colon Cancer|Recurrent Rectal Cancer|Stage IV Colon Cancer|Stage IV Rectal Cancer July 2007 Phase 2
    NCT00560352 Bristol-Myers Squibb Multiple Myeloma February 2008 Phase 1
    NCT02661113 M.D. Anderson Cancer Center|Bristol-Myers Squibb Glioblastoma|CNS Disease|Brain Diseases May 2009 Phase 2
    NCT00895960 M.D. Anderson Cancer Center|Bristol-Myers Squibb Glioblastoma|CNS Disease|Brain Diseases May 2009 Phase 1
    NCT00859937 National Cancer Institute (NCI) High-grade Salivary Gland Mucoepidermoid Carcinoma|Low-grade Salivary Gland Mucoepidermoid Carcinoma|Recurrent Salivary Gland Cancer|Salivary Gland Acinic Cell Tumor|Salivary Gland Adenocarcinoma|Salivary Gland Adenoid Cystic Carcinoma|Salivary Gland Anaplastic Carcinoma|Salivary Gland Malignant Mixed Cell Type Tumor|Salivary Gland Poorly Differentiated Carcinoma|Salivary Gland Squamous Cell Carcinoma|Stage IV Salivary Gland Cancer March 2009 Phase 2
    NCT02744768 Gruppo Italiano Malattie EMatologiche dell'Adulto Acute Lymphoblastic Leukemia December 2016 Phase 2
    NCT01593254 Bristol-Myers Squibb|ICON Clinical Research|PPD|Molecular MD|MultiPharma|Q2 solutions|Donald E. Morisky|MD Anderson Symptom Inventory (MDASI-CML)|OBiS, Inc|Steering Committee Chronic Phase Chronic Myeloid Leukemia October 29, 2012 Phase 2
    NCT00920868 Herbert Hurwitz, MD|Bristol-Myers Squibb|Duke University Solid Tumor|Metastatic Colorectal Cancer May 2009 Phase 1
    NCT00948389 Bristol-Myers Squibb|European Organisation for Research and Treatment of Cancer - EORTC Glioblastoma October 2009 Phase 1|Phase 2
    NCT00777036 Bristol-Myers Squibb Leukemia February 2009 Phase 2
    NCT01887561 Kanto CML Study Group Myelogenous Leukemia, Chronic, Chronic Phase November 2012 Phase 2
    NCT01643278 National Cancer Institute (NCI) Gastrointestinal Stromal Tumor|Stage III Soft Tissue Sarcoma|Stage IV Soft Tissue Sarcoma July 2012 Phase 1
    NCT01999985 H. Lee Moffitt Cancer Center and Research Institute|Boehringer Ingelheim|Bristol-Myers Squibb Lung Cancer|Non-small Cell Lung Cancer (NSCLC) December 31, 2013 Phase 1
    NCT00123487 Bristol-Myers Squibb Myeloid Leukemia, Chronic, Accelerated Phase|Leukemia, Lymphoblastic, Acute, Philadelphia-Positive June 2005 Phase 3
    NCT02709083 Emory University Chronic Myelogenous Leukemia|Chronic Myeloid Leukemia|Leukemia October 2016 Phase 2
    NCT00982488 Bristol-Myers Squibb Leukemia October 2007 Phase 2
    NCT02815059 University of Utah|Janssen, LP Acute Lymphoblastic Leukemia September 2016 Phase 1
    NCT00529763 Bristol-Myers Squibb Leukemia November 30, 2007 Phase 2
    NCT02546791 Bristol-Myers Squibb Small Cell Lung Cancer January 31, 2008
    NCT02954523 Giuseppe Giaccone|AstraZeneca|Bristol-Myers Squibb|Walter Reed National Military Medical Center|Hackensack University Medical Center|Georgetown University EGFR Gene Mutation|Nonsmall Cell Lung Cancer October 2016 Phase 1|Phase 2
    NCT00345826 Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI) Leukemia November 2005 Phase 1
    NCT00598091 Duke University|Bristol-Myers Squibb Refractory Solid Tumors|Pancreatic Adenocarcinoma April 2007 Phase 1
    NCT02819804 Northwestern University|National Cancer Institute (NCI) B Acute Lymphoblastic Leukemia With t(9;22)(q34;q11.2); BCR-ABL1|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Childhood Acute Lymphoblastic Leukemia|Refractory Adult Acute Lymphoblastic Leukemia|Refractory Childhood Acute Lymphoblastic Leukemia August 2016 Phase 1
    NCT00385580 Bristol-Myers Squibb Prostate Cancer January 2007 Phase 2
    NCT03041701 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Rhabdomyosarcoma|Rhabdomyosarcoma- Alveolar|Rhabdomyosarcoma-Embryonal July 7, 2017 Phase 1|Phase 2
    NCT00371254 Bristol-Myers Squibb Breast Cancer|Metastasis December 2006 Phase 2
    NCT00482703 Bristol-Myers Squibb Myeloid Leukemia, Chronic May 2007 Phase 1|Phase 2
    NCT00918385 Duke University|Bristol-Myers Squibb Prostate Cancer May 2009 Phase 2
    NCT01030718 Bristol-Myers Squibb Chronic Myelogenous Leukemia|Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia January 2006 Phase 1|Phase 2
    NCT00744497 Bristol-Myers Squibb Prostatic Neoplasms October 2008 Phase 3
    NCT00298987 Bristol-Myers Squibb Leukemia, Myeloid, Chronic|Leukemia, Lymphocytic, Acute, L2 February 2006 Phase 2
    NCT01440998 National Cancer Institute (NCI) Endometrial Adenocarcinoma|Endometrial Adenosquamous Carcinoma|Endometrial Clear Cell Adenocarcinoma|Endometrial Mucinous Adenocarcinoma|Endometrial Serous Adenocarcinoma|Endometrial Transitional Cell Carcinoma|Endometrial Undifferentiated Carcinoma|Endometrioid Adenocarcinoma|Recurrent Uterine Corpus Carcinoma|Stage III Uterine Corpus Cancer|Stage IIIA Uterine Corpus Cancer|Stage IIIB Uterine Corpus Cancer|Stage IIIC Uterine Corpus Cancer|Stage IV Uterine Corpus Cancer|Stage IVA Uterine Corpus September 20, 2011 Phase 1
    NCT02888990 Versailles Hospital Leukemia, Lymphoblastic, Acute August 2007 Phase 2
    NCT00410813 Southwest Oncology Group|National Cancer Institute (NCI) Breast Cancer|Metastatic Cancer March 2007 Phase 2
    NCT00829647 Scripps Health|Bristol-Myers Squibb|Celgene Corporation Chronic Lymphocytic Leukemia|Leukemia January 2009 Phase 1|Phase 2
    NCT00452673 Bristol-Myers Squibb Advanced Breast Cancer June 2007 Phase 1
    NCT00324077 Bristol-Myers Squibb Myeloid Leukemia, Chronic, Chronic-Phase August 2006 Phase 1
    NCT02420717 M.D. Anderson Cancer Center|Incyte Corporation Leukemia July 2015 Phase 2
    NCT01238211 National Cancer Institute (NCI) Acute Myeloid Leukemia Arising From Previous Myelodysplastic Syndrome|Adult Acute Myeloid Leukemia With Inv(16)(p13.1q22); CBFB-MYH11|Adult Acute Myeloid Leukemia With t(16;16)(p13.1;q22); CBFB-MYH11|Adult Acute Myeloid Leukemia With t(8;21); (q22; q22.1); RUNX1-RUNX1T1|Secondary Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia December 24, 2010 Phase 2
    NCT00070499 National Cancer Institute (NCI) Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Chronic Phase of Disease August 15, 2004 Phase 2
    NCT00860158 Noah Hahn, M.D.|Bristol-Myers Squibb|Hoosier Cancer Research Network Prostate Cancer March 2009 Phase 2
    NCT00101647 Bristol-Myers Squibb Chronic Myelogenous Leukemia December 2004 Phase 2
    NCT02013648 University of Ulm Acute Myeloid Leukemia (AML) July 2014 Phase 3
    NCT00544908 City of Hope Medical Center|National Cancer Institute (NCI) Pancreatic Cancer September 2007 Phase 2
    NCT00320190 Bristol-Myers Squibb Leukemia, Myeloid, Chronic August 2006 Phase 2
    NCT02680951 Emory University Acute Myeloid Leukemia December 2015 Phase 1
    NCT00444015 H. Lee Moffitt Cancer Center and Research Institute|Bristol-Myers Squibb Non-Small-Cell Lung Carcinoma March 2007 Phase 1
    NCT00316953 National Cancer Institute (NCI) Accelerated Phase Chronic Myelogenous Leukemia|Blastic Phase Chronic Myelogenous Leukemia|Childhood Chronic Myelogenous Leukemia|Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Meningeal Chronic Myelogenous Leukemia|Recurrent Childhood Acute Lymphoblastic Leukemia|Relapsing Chronic Myelogenous Leukemia|Unspecified Childhood Solid Tumor, Protocol Specific March 2006 Phase 1
    NCT00501410 M.D. Anderson Cancer Center|Bristol-Myers Squibb Colorectal Cancer April 23, 2007 Phase 1
    NCT01685125 University of Southern California|National Cancer Institute (NCI) Hormone-resistant Prostate Cancer|Recurrent Prostate Cancer|Stage IV Prostate Cancer September 2012 Phase 2
    NCT00869401 Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI)|Bristol-Myers Squibb Brain and Central Nervous System Tumors June 2009 Phase 1|Phase 2
    NCT02494882 Memorial Sloan Kettering Cancer Center|Incyte Pharmaceuticals|Novartis Pharmaceuticals Acute Lymphoblastic Leukemia June 29, 2015 Phase 1
    NCT00101816 Bristol-Myers Squibb Chronic Myeloid Leukemia|Blast Crisis December 2004 Phase 2
    NCT00101595 Bristol-Myers Squibb Chronic Myeloid Leukemia|Leukemia, Lymphoblastic, Acute, Philadelphia-positive January 2005 Phase 2
    NCT00754325 Bristol-Myers Squibb Advanced Breast Cancer September 2008 Phase 2
    NCT00903006 M.D. Anderson Cancer Center|Bristol-Myers Squibb|Merck Sharp & Dohme Corp.|Commonwealth Foundation for Cancer Research Breast Cancer November 2009 Phase 1|Phase 2
    NCT00550615 University of Nebraska|Bristol-Myers Squibb Non-Hodgkin's Lymphoma September 2007 Phase 1|Phase 2
    NCT00892177 Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) Glioblastoma Multiforme October 2009 Phase 2
    NCT00362466 Bristol-Myers Squibb Leukemia April 2007 Phase 3
    NCT00101660 Bristol-Myers Squibb Chronic Myeloid Leukemia|Philadelphia-Positive Myeloid Leukemia February 2005 Phase 2
    NCT00872976 Bristol-Myers Squibb Chronic Lymphocytic Leukemia May 2009 Phase 1
    NCT00764309 Bristol-Myers Squibb Scleroderma January 2009 Phase 1|Phase 2
    NCT02923986 Bio-Path Holdings, Inc. Chronic Myelogenous Leukemia, Ph1-Positive November 2016 Phase 1|Phase 2
    NCT00662636 Mayo Clinic|National Cancer Institute (NCI) Unspecified Adult Solid Tumor, Protocol Specific August 2008 Phase 1
    NCT00978731 Bristol-Myers Squibb Leukemia December 2005 Phase 1
    NCT00696072 Bristol-Myers Squibb|US Oncology Research Metastatic Breast Cancer August 2008 Phase 2
    NCT01410708 AHS Cancer Control Alberta Breast Cancer Phase 2
    NCT00560391 Bristol-Myers Squibb Multiple Myeloma May 2008 Phase 1
    NCT00835679 National Cancer Institute (NCI) Liver Metastases|Mucinous Adenocarcinoma of the Colon|Mucinous Adenocarcinoma of the Rectum|Recurrent Colon Cancer|Recurrent Rectal Cancer|Signet Ring Adenocarcinoma of the Colon|Signet Ring Adenocarcinoma of the Rectum|Stage IV Colon Cancer|Stage IV Rectal Cancer December 2009 Early Phase 1
    NCT00103844 Bristol-Myers Squibb Chronic Myeloid Leukemia|Philadelphia-Positive Myeloid Leukemia February 2005 Phase 2
    NCT01173679 Massachusetts General Hospital|Dana-Farber Cancer Institute|Beth Israel Deaconess Medical Center|Bristol-Myers Squibb Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma July 2010 Phase 2
    NCT00720109 National Cancer Institute (NCI) Adult B Acute Lymphoblastic Leukemia With t(9;22)(q34;q11.2); BCR-ABL1|Childhood B Acute Lymphoblastic Leukemia With t(9;22)(q34;q11.2); BCR-ABL1|Untreated Adult Acute Lymphoblastic Leukemia|Untreated Childhood Acute Lymphoblastic Leukemia July 2008 Phase 2|Phase 3
    NCT00103701 Bristol-Myers Squibb Leukemia, Myeloid, Chronic-phase|Leukemia, Lymphoblastic, Acute, Philadelphia-positive November 2003 Phase 1
    NCT01872442 Poitiers University Hospital Chronic Phase of Chronic Myeloid Leukemia October 2013 Phase 2
    NCT02733445 Bristol-Myers Squibb Chronic Myeloid Leukemia (CML) December 2015
    NCT00349518 Bristol-Myers Squibb Chronic Myeloid Leukemia|Acute Lymphoblastic Leukemia December 2006 Phase 2|Phase 3
    NCT00788125 City of Hope Medical Center|National Cancer Institute (NCI) Brain and Central Nervous System Tumors|Childhood Germ Cell Tumor|Extragonadal Germ Cell Tumor|Kidney Cancer|Liver Cancer|Lymphoma|Neuroblastoma|Ovarian Cancer|Sarcoma|Testicular Germ Cell Tumor|Unspecified Childhood Solid Tumor, Protocol Specific September 2008 Phase 1|Phase 2
    NCT00700882 Eastern Cooperative Oncology Group|National Cancer Institute (NCI) Melanoma (Skin) May 2009 Phase 2
    NCT00454753 Bristol-Myers Squibb Leukemia May 2007
    NCT00382668 Bristol-Myers Squibb Liver Diseases October 2006
    NCT01116128 Fondazione Neoplasie Sangue Onlus Myeloma February 2008 Phase 2
    NCT00500006 Merck Sharp & Dohme Corp. Chronic Myelogenous Leukemia|Leukemia, Lymphoblastic, Acute, Philadelphia-Positive October 2007 Phase 1
    NCT00391989 Gruppo Italiano Malattie EMatologiche dell'Adulto Lymphoblastic Leukemia, Acute September 2006 Phase 2
    NCT01471106 M.D. Anderson Cancer Center|Susan G. Komen Breast Cancer Foundation|Bristol-Myers Squibb Breast Cancer January 2014 Phase 2
    NCT02523976 Institute of Hematology & Blood Diseases Hospital Acute,Leukemia, Lymphoid August 2015 Phase 2
    NCT01234935 Translational Oncology Research International Acinar Cell Adenocarcinoma of the Pancreas|Duct Cell Adenocarcinoma of the Pancreas|Recurrent Pancreatic Cancer|Stage IA Pancreatic Cancer|Stage IB Pancreatic Cancer|Stage IIA Pancreatic Cancer|Stage IIB Pancreatic Cancer|Stage III Pancreatic Cancer January 2011 Phase 2
    NCT02143414 National Cancer Institute (NCI) B Acute Lymphoblastic Leukemia|B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1|B Acute Lymphoblastic Leukemia, Philadelphia Chromosome Negative|Philadelphia Chromosome Positive|Recurrent Adult Acute Lymphoblastic Leukemia|Refractory Adult Acute Lymphoblastic Leukemia|Untreated Adult Acute Lymphoblastic Leukemia January 12, 2015 Phase 2
    NCT02890784 Prof. Dr. med. Andreas Hochhaus|University of Jena Myeloid Leukemia, Chronic August 2016 Phase 3
    NCT00390793 M.D. Anderson Cancer Center|Bristol-Myers Squibb Acute Lymphoblastic Leukemia|Leukemia September 2006 Phase 2
    NCT01260688 National Cancer Institute (NCI) Hormone-resistant Prostate Cancer|Recurrent Prostate Cancer October 2010 Phase 2
    NCT00099606 Bristol-Myers Squibb Neoplasms July 2004 Phase 1
    NCT00064233 Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI) Leukemia November 2003 Phase 1
    NCT01804985 University of Liverpool|Newcastle University|Imperial College London|University of Glasgow Chronic Myeloid Leukaemia December 2013 Phase 2
    NCT00123474 Bristol-Myers Squibb Myeloid Leukemia, Chronic, Chronic-Phase July 2005 Phase 3
    NCT00337454 Bristol-Myers Squibb Chronic Myelogenous Leukemia July 2005 Phase 1|Phase 2
    NCT00780676 M.D. Anderson Cancer Center|Bristol-Myers Squibb|AstraZeneca Breast Cancer June 2009 Phase 2
    NCT00816283 City of Hope Medical Center|National Cancer Institute (NCI) Leukemia September 2008 Phase 1
    NCT01256398 National Cancer Institute (NCI) Adult B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1|Untreated Adult Acute Lymphoblastic Leukemia December 14, 2010 Phase 2
    NCT00112775 Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI) Leukemia March 2005 Phase 2
    NCT02848131 Mayo Clinic Chronic Kidney Disease July 2016 Phase 2
    NCT03173612 Institute of Hematology & Blood Diseases Hospital Acute Myeloid Leukemia August 2016
    NCT02874989 Wake Forest University Health Sciences|Mayo Clinic Idiopathic Pulmonary Fibrosis (IPF) August 2016 Phase 1
    NCT02690922 Tongji Hospital ph+ Acute Lymphoblastic Leukemia March 2016 Phase 4
    NCT00779389 University of Pittsburgh Head and Neck Cancer|Non Small Cell Lung Cancer January 2009 Phase 1
    NCT02421926 Asan Medical Center Leukemia, Myelogenous, Chronic, BCR-ABL Positive October 2014
    NCT02652052 Mayo Clinic Stem Cell Transplant March 2016
    NCT02233049 Gustave Roussy, Cancer Campus, Grand Paris|Innovative Therapies For Children with Cancer Consortium Diffuse Intrinsic Pontine Glioma October 2014 Phase 2
    NCT00036738 Fred Hutchinson Cancer Research Center|National Cancer Institute (NCI) Adult Acute Lymphoblastic Leukemia in Remission|Blastic Phase Chronic Myelogenous Leukemia|Childhood Acute Lymphoblastic Leukemia in Remission|Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Chronic Phase Chronic Myelogenous Leukemia|Philadelphia Chromosome Positive Adult Precursor Acute Lymphoblastic Leukemia|Philadelphia Chromosome Positive Childhood Precursor Acute Lymphoblastic Leukemia|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Childhood Acute Lymphoblastic Leukemia|Relapsing Ch July 2001 Phase 2
    NCT01467986 University of Regensburg Neuroblastoma Recurrent August 2013 Phase 2
    NCT02326311 Azienda Ospedaliera Spedali Civili di Brescia Leukemia, Chronic Myeloid June 2015 Phase 3
    NCT02015728 Seattle Children's Hospital|Cures Within Reach Recurrent Childhood Brain Tumor December 2013
    NCT02750514 Bristol-Myers Squibb Advanced Cancer May 6, 2016 Phase 2
    NCT01254864 M.D. Anderson Cancer Center|Bristol-Myers Squibb|Janssen Scientific Affairs, LLC|Pfizer Prostate Cancer March 2011 Phase 2
    NCT02081378 Novartis Pharmaceuticals|Novartis Chronic Myelogenous Leukemia|Philadelphia Chromosome-positive Acute Lymphoblastic Leukemia April 25, 2014 Phase 1
    NCT02883049 National Cancer Institute (NCI) B Acute Lymphoblastic Leukemia|Bone Necrosis|Central Nervous System Leukemia|Cognitive Side Effects of Cancer Therapy|Neurotoxicity Syndrome|Pain|Ph-Like Acute Lymphoblastic Leukemia|Testicular Leukemia|Therapy-Related Toxicity|Untreated Adult Acute Lymphoblastic Leukemia|Untreated Childhood Acute Lymphoblastic Leukemia February 27, 2012 Phase 3
    NCT01990196 Jonsson Comprehensive Cancer Center Prostate Cancer September 23, 2014 Phase 2
    NCT00792948 National Cancer Institute (NCI) Adult Acute Lymphoblastic Leukemia in Remission|Adult B Acute Lymphoblastic Leukemia|Adult B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1|Adult L1 Acute Lymphoblastic Leukemia|Adult L2 Acute Lymphoblastic Leukemia|Adult T Acute Lymphoblastic Leukemia|Recurrent Adult Acute Lymphoblastic Leukemia|Untreated Adult Acute Lymphoblastic Leukemia September 1, 2009 Phase 2
    NCT00549848 St. Jude Children's Research Hospital|National Cancer Institute (NCI)|Enzon Pharmaceuticals, Inc.|National Institute of General Medical Sciences (NIGMS) Acute Lymphoblastic Leukemia October 29, 2007 Phase 3
    NCT01620216 OHSU Knight Cancer Institute|National Cancer Institute (NCI) Acute Myeloid Leukemia Arising From Previous Myelodysplastic Syndrome|Chronic Myelomonocytic Leukemia|Myelodysplastic Syndrome|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Acute Myeloid Leukemia|Refractory Adult Acute Lymphoblastic Leukemia May 2012 Phase 2
    NCT00495872 M.D. Anderson Cancer Center Solid Tumors June 2007 Phase 1
    NCT02559778 Giselle Sholler|Dell, Inc.|Beat NB Cancer Foundation|Because of Ezra|Spectrum Health Hospitals Neuroblastoma September 2015 Phase 1
    NCT02596828 University of Regensburg Pineoblastoma April 2016 Phase 2
    NCT02779283 OHSU Knight Cancer Institute|National Cancer Institute (NCI) Untreated Adult Acute Myeloid Leukemia December 2015 Phase 1
    NCT03023046 University of Washington|National Cancer Institute (NCI) Adult Acute Lymphoblastic Leukemia|Adult Lymphoblastic Lymphoma|Philadelphia Chromosome Positive February 23, 2017 Phase 2
    NCT02043587 University of California, San Diego|Leadiant Biosciences, Inc. Acute Lymphocytic Leukemia|Adult Lymphoblastic Lymphoma January 2014 Phase 2
    NCT02638428 Samsung Medical Center|Ministry of health & welfare, Republic of Korea Relapsed Pediatric Solid Tumor|Refractory Pediatric Solid Tumor|Relapsed Pediatric AML|Refractory Pediatric AML December 2015 Phase 2
    NCT01771458 Institut Curie Reccurent/Metastatic Solid Tumor Disease October 2012 Phase 2
    NCT03117751 St. Jude Children's Research Hospital|Bristol-Myers Squibb|Incyte Corporation|Shire Acute Lymphoblastic Leukemia|Acute Lymphoblastic Lymphoma March 29, 2017 Phase 2|Phase 3
    NCT02693535 American Society of Clinical Oncology|AstraZeneca|Bayer|Bristol-Myers Squibb|Eli Lilly and Company|Genentech, Inc.|Merck Sharp & Dohme Corp.|Pfizer Lymphoma, Non-Hodgkin|Multiple Myeloma|Advanced Solid Tumors March 2016 Phase 2
    NCT02465060 National Cancer Institute (NCI) Advanced Malignant Solid Neoplasm|Bladder Carcinoma|Breast Carcinoma|Cervical Carcinoma|Colon Carcinoma|Colorectal Carcinoma|Endometrial Carcinoma|Esophageal Carcinoma|Gastric Carcinoma|Glioma|Head and Neck Carcinoma|Kidney Carcinoma|Liver and Intrahepatic Bile Duct Carcinoma|Lung Carcinoma|Lymphoma|Malignant Uterine Neoplasm|Melanoma|Ovarian Carcinoma|Pancreatic Carcinoma|Plasma Cell Myeloma|Prostate Carcinoma|Rectal Carcinoma|Recurrent Bladder Carcinoma|Recurrent Breast Carcinoma|Recurrent Cer August 12, 2015 Phase 2
    NCT03020030 Dana-Farber Cancer Institute|Baxalta US Inc. Acute Lymphoblastic Leukemia, Pediatric January 2017 Phase 3
    NCT01636908 VU University Medical Center Cancer|Advanced Solid Tumors August 2011
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    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
    1 mM 2.0491 mL 10.2457 mL 20.4914 mL
    5 mM 0.4098 mL 2.0491 mL 4.0983 mL
    10 mM 0.2049 mL 1.0246 mL 2.0491 mL
    Kinase Assay
    [1]

    Kinase assays using wild-type and mutant glutathione S-transferase (GST)-Abl fusion proteins (c-Abl amino acids 220-498) are done with minor alterations. GST-Abl fusion proteins are released from glutathione-Sepharose beads before use; the concentration of ATP is 5 μM. Immediately before use in kinase autophosphorylation and in vitro peptide substrate phosphorylation assays, GST-Abl kinase domain fusion proteins are treated with LAR tyrosine phosphatase. After 1-hour incubation at 30°C, LAR phosphatase is inactivated by addition of sodium vanadate (1 mM). Immunoblot analysis comparing untreated GST-Abl kinase to dephosphorylated GST-Abl kinase is routinely done using phosphotyrosine-specific antibody 4G10 to confirm complete (>95%) dephosphorylation of tyrosine residues and c-Abl antibody CST 2862 to confirm equal loading of GST-Abl kinase. The inhibitor concentration ranges for IC50 determinations are 0 to 5,000 nM (Imatinib and AMN107) or 0 to 32 nM (Dasatinib). The Dasatinib concentration range is extended to 1,000 nM for mutant T315I. These same inhibitor concentrations are used for the in vitro peptide substrate phosphorylation assays. The three inhibitors are tested over these same concentration ranges against GST-Src kinase and GST-Lyn kinase. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    Dasatinib is dissolved in DMSO (10 mM) and stored, and then diluted with appropriate media before use[1].

    Ba/F3 cell lines are plated in triplicate and incubated with escalating concentrations of Imatinib, AMN107, or Dasatinib for 72 hours. Proliferation is measured using a methanethiosulfonate-based viability assay (CellTiter96 Aqueous One Solution Reagent). IC50 and IC90 values are reported as the mean of three independent experiments done in quadruplicate. The inhibitor concentration ranges for IC50 and IC90determinations are 0 to 2,000 nM (Imatinib and AMN107) or 0 to 32 nM (Dasatinib). The imatinib concentration range is extended to 6,400 nM for mutants with IC50>2,000 nM. The Dasatinib concentration range is extended to 200 nM for mutant T315I. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3][4]

    Dasatinib is prepared in 80 mM sodium citrate buffer, pH 3.0 (Mice)[3].
    Dasatinib is prepared in 0.5% methylcellulose (Rat)[4].

    Mice[3]
    Male athymic nude mice (25 grams; 5-week old) are used. Dasatinib (50 mg/kg) is prepared for daily oral gavage (5 d/wk) in 80 mM sodium citrate buffer, pH 3.0. For the orthotopic murine model, mice are randomized on day 10 based on bioluminescence activity to receive drug or vehicle. In the metastatic murine model, mice receives dasatinib or vehicle, as described earlier, starting 2 days before intracardiac injection (pretreatment), or on day 11 following randomization (posttreatment).
    Rat[4]
    Dasatinib is dosed to male Wistar-Han (WH) rats at 50 mg/kg orally in 0.5% methylcellulose. The automated rat blood collection device is programmed to collect 200 μL of blood at predetermined intervals. At each time point, the accusampler is programmed to directly spot 20 μL of blood twice (two spots) onto the DBS card. The remaining 160 μL of liquid blood is collected into sodium EDTA-containing tubes. Plasma samples are obtained after immediate centrifugation of blood at 11,000 rpm for 5 min. The plasma samples are stored at −80°C until analyses. The DBS samples are dried under room temperature for a minimum of 2 h and stored in a plastic bag in the dessicator until sample analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.84%

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