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

Nilotinib (Synonyms: Tasigna; AMN107)

Cat. No.: HY-10159 Purity: 99.93%
Data Sheet SDS Handling Instructions

Nilotinib is a second generation tyrosine kinase inhibitor (TKI), is significantly more potent against BCR-ABL than Imatinib, and is active against many Imatinib-resistant BCR-ABL mutants.

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

Nilotinib Chemical Structure

CAS No. : 641571-10-0

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Customer Review

Other Forms of Nilotinib:

    Nilotinib purchased from MCE. Usage Cited in: Leuk Lymphoma. 2015;56(8):2416-23.

    Cell cycle analysis of HT93A cells by flow cytometry. Cells are treated with 100 nM Nilotinib and 50 ng/mL G-CSF alone or in combination for 48 h before the cell cycle is analyzed. Nilotinib treatment increases the fraction of cells in G0/G1 phase and decreased the S+G2/M-phase fraction.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Nilotinib is a second generation tyrosine kinase inhibitor (TKI), is significantly more potent against BCR-ABL than Imatinib, and is active against many Imatinib-resistant BCR-ABL mutants.

    IC50 & Target

    Bcr-Abl[1]

    In Vitro

    The novel, selective Abl inhibitor, Nilotinib (AMN107), is designed to interact with the ATP-binding site of BCR-ABL with a higher affinity than Imatinib. In addition to being significantly more potent compared with Imatinib (IC50<30 nM), Nilotinib also maintains activity against most of the BCR-ABL point mutants that confer Imatinib resistance[1]. Nilotinib demonstrates significant antitumor efficacy against GIST xenograft lines and Imatinib-resistant GIST cell lines. The parent cell lines GK1C and GK3C show Imatinib sensitivity with IC50 of 4.59±0.97 µM and 11.15±1.48 µM, respectively. The Imatinib-resistant cell lines GK1C-IR and GK3C-IR show Imatinib resistance with IC50 values of 11.74±0.17 µM (P<0.001) and 41.37±1.07 µM (P<0.001), respectively[2].

    In Vivo

    The percentage of tumor growth inhibition (TGI) is 83.8% for Imatinib and 69.6% for Nilotinib in the GK1X xenograft line (n.s.). In the GK2X xenograft line, TGI is 83.0% for Imatinib and 85.3% for Nilotinib (n.s.). Additionally, the GK3X xenograft line TGI is 31.1% for Imatinib and 47.5% for Nilotinib (n.s.). These results suggest that, except for the GK1X xenograft line, Nilotinib shows equivalent or higher antitumor effects than Imatinib[2]. Nilotinib has a significant healing effect on the macroscopic and microscopic pathologic scores and ensures considerable mucosal healing in the indomethacin-induced enterocolitis rat model. While Nilotinib decreased the PDGFR α and β levels and apoptotic scores in the colon, it did not have a significant effect on the weight and TNF-α levels. Further experimental investigations could provide more definitive evidence for humans[3].

    Clinical Trial
    NCT Number Sponsor Condition Start Date Phase
    NCT00135005 Novartis Pharmaceuticals|Novartis Gastrointestinal Stromal Tumors August 2005 Phase 1
    NCT00264160 Novartis Pharmaceuticals|Novartis Leukemia, Myeloid, Chronic May 2006 Phase 2|Phase 3
    NCT00302016 Novartis Pharmaceuticals|Novartis Chronic Myeloid Leukemia January 2006
    NCT00718562 Novartis Pharmaceuticals|Novartis Gastrointestinal Stromal Tumors September 2008 Phase 2
    NCT01735955 Novartis Pharmaceuticals|Novartis GIST and CML March 29, 2013 Phase 4
    NCT00633295 Novartis Pharmaceuticals|Novartis Gastrointestinal Stromal Tumors (GIST) June 2008 Phase 2
    NCT01744665 Novartis Pharmaceuticals|Novartis CML August 12, 2013 Phase 2
    NCT01605981 Novartis Pharmaceuticals|Novartis Chronic Myeloid Leukemia (CML) February 2014 Phase 4
    NCT00519090 Novartis Pharmaceuticals|Novartis Myelogenous Leukemia October 2007 Phase 3
    NCT00785785 Novartis Pharmaceuticals|Novartis Gastrointestinal Stromal Tumor (GIST) March 2009 Phase 3
    NCT00135005 Novartis Pharmaceuticals|Novartis Gastrointestinal Stromal Tumors August 2005 Phase 1
    NCT00264160 Novartis Pharmaceuticals|Novartis Leukemia, Myeloid, Chronic May 2006 Phase 2|Phase 3
    NCT00302016 Novartis Pharmaceuticals|Novartis Chronic Myeloid Leukemia January 2006
    NCT00718562 Novartis Pharmaceuticals|Novartis Gastrointestinal Stromal Tumors September 2008 Phase 2
    NCT01735955 Novartis Pharmaceuticals|Novartis GIST and CML March 29, 2013 Phase 4
    NCT00633295 Novartis Pharmaceuticals|Novartis Gastrointestinal Stromal Tumors (GIST) June 2008 Phase 2
    NCT01744665 Novartis Pharmaceuticals|Novartis CML August 12, 2013 Phase 2
    NCT01605981 Novartis Pharmaceuticals|Novartis Chronic Myeloid Leukemia (CML) February 2014 Phase 4
    NCT00519090 Novartis Pharmaceuticals|Novartis Myelogenous Leukemia October 2007 Phase 3
    NCT00785785 Novartis Pharmaceuticals|Novartis Gastrointestinal Stromal Tumor (GIST) March 2009 Phase 3
    NCT02086487 King Abdullah International Medical Research Center|Novartis Myeloid Leukemia, Chronic March 2013 Phase 4
    NCT02954978 Georgetown University Parkinson Disease|Parkinsons Disease With Dementia January 2017 Phase 2
    NCT01562847 Seoul St. Mary's Hospital|Novartis Chronic Myeloid Leukemia July 2011 Phase 2
    NCT00980018 Novartis Pharmaceuticals|Novartis Chronic Myelogenous Leukemia December 2009 Phase 4
    NCT01316250 American University of Beirut Medical Center Chronic Myelogenous Leukemia August 2010
    NCT01698905 Novartis Pharmaceuticals|Novartis Chronic Myeloid Leukemia December 20, 2012 Phase 2
    NCT00976612 Asan Medical Center Gastrointestinal Stromal Tumors January 2009
    NCT01856283 Niguarda Hospital Leukemia, Myeloid, Chronic-Phase March 2013 Phase 2
    NCT01131325 Novartis Pharmaceuticals|Novartis CML|Philadelphia Chromosome Positive (Ph+)|Chronic Myelogenous Leukemia Chronic Phase(CML-CP) Patients With Low Imatinib Trough Levels October 2010 Phase 4
    NCT02201459 Hospices Civils de Lyon|Novartis Chronic Myeloid Leukemia August 2014 Phase 3
    NCT01810718 Gruppo Italiano Trapianto di Midollo Osseo Chronic Graft Versus Host Disease November 2011 Phase 1
    NCT01690065 Ulsan University Hospital|The Korean Society of Hematology CML working party Chronic Myeloid Leukemia in Myeloid Blast Crisis|Untreated Adult Acute Myeloid Leukemia September 2012 Phase 2
    NCT02947893 Georgetown University Alzheimer's Disease January 2017 Phase 2
    NCT01395121 Institute of Cancer Research, United Kingdom|Royal Marsden NHS Foundation Trust Mucosal Lentiginous Melanoma|Acral Lentiginous Malignant Melanoma December 2009 Phase 2
    NCT00788775 Dana-Farber Cancer Institute|Brigham and Women's Hospital|Beth Israel Deaconess Medical Center|Massachusetts General Hospital|Novartis Mucosal Lentiginous Melanoma|Acral Melanoma|Melanoma January 2009 Phase 2
    NCT01089595 Fox Chase Cancer Center|Novartis GIST|Metastatic Disease February 2009 Phase 2
    NCT02587169 Broto, Javier Martín, M.D. Retroperitoneal Liposarcoma|Retroperitoneal Leiomyosarcoma|Chondrosarcoma January 2012 Phase 1|Phase 2
    NCT01270893 M.D. Anderson Cancer Center|Novartis Gastrointestinal Cancer January 2011 Phase 2
    NCT01222143 University Health Network, Toronto|Novartis Pharmaceuticals Acute Myeloid Leukemia October 2010 Phase 1|Phase 2
    NCT02108951 Novartis Pharmaceuticals|Novartis Philidelphia Positive Chronic Myeloid Leukaemia July 2014 Phase 3
    NCT01207492 Andrew J. Wagner, MD, PhD|Brigham and Women's Hospital|Massachusetts General Hospital|Novartis|Dana-Farber Cancer Institute Pigmented Villonodular Synovitis|Diffuse-type Giant Cell Tumor|Tenosynovial Giant Cell Tumor September 2010 Phase 2
    NCT01528085 Johann Wolfgang Goethe University Hospital Philadelphia Chromsome Positive Acute Lymphoblastic Leukemia January 2012 Phase 2
    NCT02379416 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Solid Tumors February 20, 2015 Phase 1
    NCT01657604 University of Jena Chronic Myeloid Leukemia August 2012 Phase 3
    NCT01252017 National Taiwan University Hospital Patients Who Have Received Allo-HSCT November 2010 Phase 2
    NCT00129740 M.D. Anderson Cancer Center|Novartis Leukemia, Myelogenous, Chronic June 27, 2005 Phase 2
    NCT01819389 Hospital Universitario Dr. Jose E. Gonzalez|Novartis Pharmaceuticals Leukemia, Myeloid, Chronic, BCR-ABL Positive October 2012 Phase 3
    NCT01043874 Novartis Pharmaceuticals|Novartis Philadelphia Chromosome Positive|Chronic Myelogenous Leukemia in Chronic Phase December 2009 Phase 4
    NCT01061177 Novartis Pharmaceuticals|Novartis CML in Chronic Phase May 2010 Phase 4
    NCT00471328 Novartis Pharmaceuticals|Novartis Gastrointestinal Stromal Tumors March 2007 Phase 3
    NCT01863745 Novartis Pharmaceuticals|Novartis Gastrointestinal Stromal Tumors June 25, 2013 Phase 2
    NCT01099514 Samsung Medical Center Metastatic Melanoma With KIT Aberration August 2009 Phase 2
    NCT01743989 Novartis Pharmaceuticals|Novartis Leukemia, Myeloid, Ph1-Positive April 15, 2013 Phase 3
    NCT02281474 Georgetown University Parkinson's Disease|Parkinson's Disease Dementia|Diffuse Lewy Body Disease November 2014 Phase 1
    NCT01914484 University Health Network, Toronto|Novartis Chronic Phase Chronic Myeloid Leukemia|Accelerated Phase Chronic Myeloid Leukemia|Blastic Phase Chronic Myeloid Leukemia|Philadelphia Positive Acute Lymphoblastic Leukemia|Resistant to Tyrosine Kinase Inhibitor Therapy August 2013 Phase 1|Phase 2
    NCT00751036 Novartis Pharmaceuticals|Novartis Gastrointestinal Stromal Tumors June 2009 Phase 3
    NCT01866553 VU University Medical Center|Uppsala University Hospital|Novartis|Merck Sharp & Dohme Corp. Chronic Myeloid Leukemia April 2013 Phase 2
    NCT02973711 University of Michigan Cancer Center Leukemia, Chronic Myeloid May 22, 2017 Phase 1|Phase 2
    NCT01179737 Novartis Pharmaceuticals|Novartis Pulmonary Arterial Hypertension July 2010 Phase 2
    NCT01784068 Novartis Pharmaceuticals|Novartis Chronic Myelogenous Leukemia March 4, 2013 Phase 2
    NCT00844298 Asan Medical Center Leukemia January 2009 Phase 2
    NCT00418626 Novartis Pharmaceuticals|Novartis Healthy November 2006 Phase 1
    NCT01166139 Hospital for Special Surgery, New York|Rudolph Rupert Scleroderma Program|Novartis Pharmaceuticals Systemic Sclerosis July 2010 Phase 2
    NCT00782834 Fox Chase Cancer Center Gastrointestinal Stromal Tumors July 2008 Phase 2
    NCT00418756 Novartis Pharmaceuticals|Novartis Healthy October 2006 Phase 1
    NCT01702064 H. Lee Moffitt Cancer Center and Research Institute|Incyte Corporation Chronic Phase Chronic Myeloid Leukemia February 21, 2013 Phase 1
    NCT01400074 Seoul St. Mary's Hospital|Novartis Chronic Myeloid Leukemia January 2009 Phase 3
    NCT01456676 Novartis Pharmaceuticals|Novartis Philadelphia Chromosome Positive Chronic Myelogenous Leukemia January 2012 Phase 1
    NCT02253277 Novartis Pharmaceuticals|Novartis Chronic Myeloid Leukemia February 18, 2015 Phase 1|Phase 2
    NCT00750659 Sheba Medical Center Chronic Myeloid Leukemia|Acute Lymphoblastic Leukemia|Stem Cell Transplantation July 2009 Phase 2
    NCT00418769 Novartis Pharmaceuticals|Novartis Healthy June 2006 Phase 1
    NCT01407198 Massachusetts General Hospital Chordoma August 2011 Phase 1
    NCT02546674 Novartis Pharmaceuticals|Novartis Chronic Myeloid Leukemia February 20, 2016 Phase 4
    NCT01254188 Novartis Pharmaceuticals|Novartis Chronic Myeloid Leukemia April 2011 Phase 3
    NCT02001818 Australasian Leukaemia and Lymphoma Group|Merck Sharp & Dohme (Australia) Pty Limited|Novartis Pharmaceuticals Chronic Myeloid Leukaemia April 2014 Phase 2
    NCT03079505 Hamad Medical Corporation Chronic Myeloid Leukemia - Chronic Phase June 2017 Phase 3
    NCT01206088 Novartis Pharmaceuticals|Novartis CML|Nilotinib|Imatinib Resistant|Imatinib Intolerant February 2009 Phase 4
    NCT01155817 Stanford University|Novartis Bone Marrow Transplant Failure|Lymphoma, Non-Hodgkin|Lymphoma, T-Cell, Peripheral August 2010 Phase 1
    NCT01844765 Novartis Pharmaceuticals|Children's Oncology Group|Innovative Therapies For Children with Cancer Consortium|Novartis Leukemia|Leukemia,Pediatric|Leukemia, Myleiod|Leukemia, Mylegenous, Chronic|Leukemia, Mylegenous, Accelerated|BCR-ABL Positive|Myeloproliferative Disorder|Bone Marrow Disease|Hematologic Diseases|Neoplastic Processes|Imatinib|Dasatinib|Enzyme Inhibitor|Protein Kinase Inhibitor August 20, 2013 Phase 2
    NCT02891395 University Hospital, Lille|Novartis Graft Versus Host Disease December 2012 Phase 2
    NCT00756509 Novartis Pharmaceuticals|Novartis Gastrointestinal Stromal Tumors August 29, 2008 Phase 4
    NCT02225574 M.D. Anderson Cancer Center|Array BioPharma Leukemia March 11, 2015 Phase 1|Phase 2
    NCT00644878 Novartis Pharmaceuticals|Novartis Chronic Myelogenous Leukemia - Chronic Phase October 2008 Phase 4
    NCT01884922 Gustave Roussy, Cancer Campus, Grand Paris Refractory Low-grade Gliomas|Recurrent Low-grade Gliomas May 2013 Phase 1
    NCT01289028 Novartis Pharmaceuticals|Novartis Gastrointestinal Stromal Tumors November 2008 Phase 3
    NCT01168050 Assistance Publique - Hôpitaux de Paris Malignant Skin Melanoma T0|Stage III Melanoma|Stage IV Melanoma|Amplification July 2010 Phase 2
    NCT00802841 Novartis Pharmaceuticals|Novartis Chronic Myelogenous Leukemia May 2009 Phase 3
    NCT02353728 Weill Medical College of Cornell University|Novartis Pharmaceuticals Chronic Myeloid Leukemia January 2015 Phase 2
    NCT03228303 Assiut University Chronic Myeloid Leukemia August 1, 2017 Early Phase 1
    NCT02917720 European LeukemiaNet|Heidelberg University|Ludwig-Maximilians - University of Munich Chronic Myeloid Leukemia October 2016 Phase 2
    NCT02774512 Institut Bergonié|Novartis Pharmaceuticals Colon Cancer May 2016 Early Phase 1
    NCT02272777 Novartis Pharmaceuticals|Novartis Leukemia July 17, 2014 Phase 3
    NCT00441155 Novartis Pharmaceuticals|Novartis Gastrointestinal Stromal Tumors November 2006 Phase 1
    NCT01077544 Novartis Pharmaceuticals|Novartis Chronic Myeloid Leukemia|Acute Lymphoblastic Leukemia April 2011 Phase 1
    NCT00718263 Novartis Pharmaceuticals|Novartis Myelogenous Leukemia, Chronic April 2008 Phase 3
    NCT01368523 Novartis Pharmaceuticals|Novartis Chronic Myelogenous Leukemia December 2008 Phase 4
    NCT01535391 Gruppo Italiano Malattie EMatologiche dell'Adulto Chronic Myeloid Leukemia January 2012 Phase 3
    NCT01774630 University Hospital, Bordeaux Leukemia, Myelogenous, Chronic, BCR-ABL Positive April 2013 Phase 2
    NCT02709083 Emory University Chronic Myelogenous Leukemia|Chronic Myeloid Leukemia|Leukemia October 2016 Phase 2
    NCT00471497 Novartis Pharmaceuticals|Novartis Myelogenous Leukemia, Chronic July 31, 2007 Phase 3
    NCT01126892 Novartis Pharmaceuticals|Novartis Chronic Myeloid Leukemia January 2009 Phase 3
    NCT01294618 Hospices Civils de Lyon Chronic Myelogenous Leukemia March 2011 Phase 2
    NCT01140568 David Piccioni, M.D., Ph.D|Novartis|University of California, San Diego Glioma May 2010 Phase 2
    NCT01110668 Novartis Pharmaceuticals|Novartis Gastrointestinal Stromal Tumor September 2008 Phase 2
    NCT01279473 Novartis Pharmaceuticals|Novartis Chronic Myelogenous Leukemia|Acute Lymphoblastic Leukemia August 2005 Phase 1|Phase 2
    NCT02115386 Novartis Pharmaceuticals|Novartis Philadelphia Positive (Ph+) Chronic Myeloid Leukemia December 2015 Phase 3
    NCT01220648 Novartis Pharmaceuticals|Novartis Chronic Myeloid Leukemia April 2012 Phase 1
    NCT00762632 Technische Universität München Acute Myeloid Leukemia December 2007 Phase 1|Phase 2
    NCT00732888 Jan Beumer|Novartis Pharmaceuticals|University of Pittsburgh Healthy November 2008 Phase 1
    NCT02627677 Ariad Pharmaceuticals Chronic Phase Chronic Myeloid Leukemia December 2015 Phase 3
    NCT00760877 Novartis Pharmaceuticals|Novartis CHRONIC MYELOGENOUS LEUKEMIA June 2009 Phase 3
    NCT00905398 Rony Schaffel|Universidade Federal do Rio de Janeiro Precursor B-Cell Lymphoblastic Leukemia-Lymphoma|Acute Lymphoblastic Leukemia May 2009 Phase 1|Phase 2
    NCT01806571 Mayo Clinic|National Cancer Institute (NCI) Untreated Adult Acute Myeloid Leukemia March 12, 2015 Phase 2
    NCT02174445 Prof. Dr. Nikolas von Bubnoff|Novartis|University Hospital Freiburg Chronic Myeloid Leukemia March 2014 Phase 3
    NCT01860456 University of Pisa Chronic Myeloid Leukemia May 2013
    NCT01227577 Novartis Pharmaceuticals|Novartis Chronic Myelogenous Leukemia in Chronic Phase November 2010 Phase 4
    NCT00702403 Fred Hutchinson Cancer Research Center|National Cancer Institute (NCI) Accelerated Phase Chronic Myelogenous Leukemia|Adult Acute Lymphoblastic Leukemia in Remission|Blastic Phase Chronic Myelogenous Leukemia|Childhood Acute Lymphoblastic Leukemia in Remission|Childhood Chronic Myelogenous Leukemia|Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Chronic Phase Chronic Myelogenous Leukemia|Philadelphia Positive Adult Acute Lymphoblastic Leukemia|Philadelphia Positive Childhood Acute Lymphoblastic Leukemia|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Childho April 2008 Phase 1|Phase 2
    NCT01275196 Novartis Pharmaceuticals|Novartis Chronic Myeloid Leukemia April 2011 Phase 3
    NCT01887522 Gustave Roussy, Cancer Campus, Grand Paris|Innovative Therapies For Children with Cancer Consortium Refractory Low-grade Gliomas|Recurrent Low-grade Gliomas June 2016 Phase 2
    NCT00481052 Gruppo Italiano Malattie EMatologiche dell'Adulto Chronic Myeloid Leukemia June 2007 Phase 2
    NCT00413270 Novartis Pharmaceuticals|Novartis Chronic Myelogenous Leukemia December 2006
    NCT00905593 Novartis Pharmaceuticals|Novartis Chronic Myeloid Leukemia September 2008
    NCT02389920 Samsung Medical Center Leukemia, Chronic Myeloid April 2015 Phase 4
    NCT01201538 University Health Network, Toronto|Novartis Growing Vestibular Schwannomas October 2010 Phase 2
    NCT02733445 Bristol-Myers Squibb Chronic Myeloid Leukemia (CML) December 2015
    NCT00809211 Cancer Trials Ireland Leukemia October 2008 Phase 2
    NCT01871311 Georgetown University|Novartis Colorectal Cancer|Head and Neck Cancer May 2014 Phase 1
    NCT00786812 Novartis Pharmaceuticals|Novartis Chronic Myeloid Leukemia August 2008 Phase 4
    NCT03205488 Northwestern University|University of Rochester|University of Iowa|Michael J. Fox Foundation for Parkinson's Research Parkinson Disease September 2017 Phase 2
    NCT00384228 Novartis Pharmaceuticals|Novartis Chronic Myelogenous Leukemia|Acute Lymphoblastic Leukemia (Philadelphia Chromosome Positive) May 2005 Phase 1|Phase 2
    NCT01804985 University of Liverpool|Newcastle University|Imperial College London|University of Glasgow Chronic Myeloid Leukaemia December 2013 Phase 2
    NCT01025505 Gruppo Italiano Malattie EMatologiche dell'Adulto Treatment|Stem Cell Transplantation June 2012 Phase 2
    NCT01670084 Mayo Clinic B-cell Adult Acute Lymphoblastic Leukemia|Blastic Phase Chronic Myelogenous Leukemia|Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Philadelphia Chromosome Positive Adult Precursor Acute Lymphoblastic Leukemia|Untreated Adult Acute Lymphoblastic Leukemia December 2012 Phase 2
    NCT01028222 Novartis Pharmaceuticals|Novartis Melanoma June 2010 Phase 2
    NCT00769327 Gruppo Italiano Malattie EMatologiche dell'Adulto Leukemia February 2009 Phase 2
    NCT02602314 Gruppo Italiano Malattie EMatologiche dell'Adulto Chronyc Myeloid Leukemia December 2016 Phase 4
    NCT03214718 Assiut University Chronic Myeloid Leukemia Patients August 5, 2017
    NCT02326311 Azienda Ospedaliera Spedali Civili di Brescia Leukemia, Chronic Myeloid June 2015 Phase 3
    NCT02421926 Asan Medical Center Leukemia, Myelogenous, Chronic, BCR-ABL Positive October 2014
    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
    NCT02081378 Novartis Pharmaceuticals|Novartis Chronic Myelogenous Leukemia|Philadelphia Chromosome-positive Acute Lymphoblastic Leukemia April 25, 2014 Phase 1
    NCT00109707 Novartis Pharmaceuticals|Novartis Chronic Myelogenous Leukemia|Acute Lymphoblastic Leukemia (Philadelphia Chromosome Positive)|Hypereosinophilic Syndrome|Systemic Mastocytosis May 2004 Phase 1|Phase 2
    NCT02611492 Assistance Publique - Hôpitaux de Paris Philadelphia Chromosome Positive Adult Acute Lymphoblastic Leukemia April 2016 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
    NCT02029001 Centre Leon Berard|National Cancer Institute, France Malignant Solid Neoplasms February 2014 Phase 2
    NCT02779283 OHSU Knight Cancer Institute|National Cancer Institute (NCI) Untreated Adult Acute Myeloid Leukemia December 2015 Phase 1
    NCT02925234 The Netherlands Cancer Institute|Amgen|AstraZeneca|Bayer|Bristol-Myers Squibb|Novartis|Roche Pharma AG Cancer|Tumors|Neoplasm|Neoplasia August 2016 Phase 2
    NCT01275586 Indiana University|Novartis Neurofibromatosis|NF1|Neurofibromas January 2011 Early Phase 1
    NCT01223898 Novartis Pharmaceuticals|Novartis Chronic Myeloid Leukemia June 2010 Phase 1
    NCT01261429 Centre Leon Berard|Ministry of Health, France Pigmented Villonodular Synovitis December 2010 Phase 2
    NCT01289054 Novartis Pharmaceuticals|Novartis All Indications for Glivec/Gleevec and Tasigna January 2011
    NCT02068898 XSpray Microparticles Healthy December 2013 Phase 1
    NCT01274351 Novartis Pharmaceuticals|Novartis Chronic Myelogenous Leukemia January 25, 2011 Phase 2
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    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
    1 mM 1.8885 mL 9.4425 mL 18.8850 mL
    5 mM 0.3777 mL 1.8885 mL 3.7770 mL
    10 mM 0.1889 mL 0.9443 mL 1.8885 mL
    Cell Assay
    [2]

    Nilotinib is prepared in 100% DMSO (10 mM) and then diluted to final concentration in medium[2].

    The human GIST cell lines GK1C and GK3C, and the Imatinib-resistant cell lines GK1C-IR and GK3C-IR are plated in 96-well microplates and cultured for 12 h before exposure to Imatinib (1-100 µM) or Nilotinib (1-100 µM) for 72 h. The cells are quantified by the WST-8 assay. The optical density (OD) is determined with Sunrise rainbow. The rate of inhibition is calculated as follows: % of inhibition=(OD of treated group-blank)/(OD of control group-blank)×100%. The concentration of tested drugs resulting in 50% growth inhibition (IC50) is calculated[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2][3]

    Nilotinib is dissolved in N-methyl-2-pyrrolidone (NMP) at 100 mg/mL and diluted 1:10 (10 plus 90 v/v) with polyethylene glycol 300 (PEG300) to final 10 mg/mL (Mice)[2].
    Nilotinib is prepared in DMSO and then dioluted with saline (Rat)[3].

    Mice[2]
    The GIST xenograft lines GK1X, GK2X and GK3X in nude mice are used. These xenograft lines are maintained by continual passage in BALB/cSLc-nu/nu mice. Mice bearing GK1X, GK2X and GK3X tumors (6-8 mice per group) are treated daily with vehicle or 40 mg/kg Imatinib or Nilotinib for 4 weeks. Tumor volume (TV) is determined from caliper measurements of tumor length (L) and width (w) according to the formula LW2/2. TV is determined every two to three days and on the day of evaluation. Mice are sacrificed and the percentage of tumor growth inhibition (TGI) is calculated as follows: TGI (%)=[1-(mean of treatment group tumor volume on evaluation day-mean of treatment group tumor volume on day 1)/(mean of control group tumor volume on evaluation day-mean of control group tumor volume on day 1)]×100.
    Rat[3]
    Female Wistar albino rats, weighing 226-243 g (mean weight, 241.09 g), for use in this study. Nilotinib, administered 20 mg/kg/d in two divided doses, is administered to the Nilotinib group of rats (n=7) for 13 d through an orogastric tube, beginning on the same day as indomethacin administration. Blood and tissue samples for pathological examination are obtained from all rats under ether anesthesia at the end of the 13-d period. All animals are then sacrificed by decapitation. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.93%

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    Nilotinib
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