1. Apoptosis
  2. Bcl-2 Family

Navitoclax (Synonyms: ABT-263)

Cat. No.: HY-10087 Purity: 99.34%
Data Sheet SDS Handling Instructions

Navitoclax is a potent and orally bioavailable Bcl-2 family protein inhibitor that binds with high affinity (Ki < 1 nM) to multiple anti-apoptotic Bcl-2 family proteins including Bcl-xL, Bcl-2 and Bcl-w.

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

Navitoclax Chemical Structure

CAS No. : 923564-51-6

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Description

Navitoclax is a potent and orally bioavailable Bcl-2 family protein inhibitor that binds with high affinity (Ki < 1 nM) to multiple anti-apoptotic Bcl-2 family proteins including Bcl-xL, Bcl-2 and Bcl-w.

IC50 & Target

Ki: < 1 nM (Bcl-xL), < 1 nM (Bcl-2), < 1 nM (Bcl-w)

In Vitro

Navitoclax (ABT-263) is active against approximately one-half of the cell lines of the PPTP in vitro panel. The median IC50 for all of the lines in the panel is 1.91 µM[1]. Navitoclax in combination with chemotherapy agents leads most ovarian cancer cell lines a synergistic response, and enhances the caspase activation at all paclitaxel doses tested in both SK-OV-3 and IGROV-1 cell lines[2].

In Vivo

Navitoclax (100 mg/kg/day, p.o.) also improves responses to bendamustine-rituximab (BR) in a subset of tumours in mice xenograft[3].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00788684 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie CD20-Positive Lymphoid Malignancies|Chronic Lymphoid Leukemia|Hematological Malignancies|Non-Hodgkin's Lymphoma July 28, 2009 Phase 1
NCT01021358 Abbott Lymphoma|Chronic Lymphocytic Leukemia|Solid Tumors January 2010 Phase 1
NCT00887757 Abbott|Genentech, Inc. Solid Tumors September 2009 Phase 1
NCT02591095 Centre Francois Baclesse|ARCAGY/ GINECO GROUP|French Cancer Research Hospital Program Platinum-resistant or Refractory Ovarian Cancer January 2016 Phase 2
NCT00891605 Abbott|Genentech, Inc. Solid Tumors July 2009 Phase 1
NCT00918450 Abbott|Genentech, Inc. B-cell Chronic Lymphocytic Leukemia March 2010 Phase 2
NCT00868413 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Chronic Lymphocytic Leukemia November 2009 Phase 1
NCT00888108 Abbott|Genentech, Inc. Solid Tumor July 2009 Phase 1
NCT00878449 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Solid Tumors October 2009 Phase 1
NCT00406809 AbbVie (prior sponsor, Abbott)|AbbVie Chronic Lymphoid Leukemia|Lymphoid Malignancies|Non-Hodgkin's Lymphoma|Follicular Lymphoma|Mantle Cell Lymphoma|Peripheral T-cell Lymphoma November 2006 Phase 2
NCT00743028 Abbott|Genentech, Inc. Chronic Lymphocytic Leukemia|Lymphomas|Leukemias August 2008 Phase 1
NCT00481091 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Chronic Lymphocytic Leukemia July 25, 2007 Phase 2
NCT00445198 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Small Cell Lung Cancer|Small Cell Lung Carcinoma April 2007 Phase 1|Phase 2
NCT01009073 AbbVie (prior sponsor, Abbott)|AbbVie Solid Tumors October 2009 Phase 1
NCT01087151 Genentech, Inc.|AbbVie (prior sponsor, Abbott) Chronic Lymphocytic Leukemia August 2010 Phase 2
NCT01828476 Rutgers, The State University of New Jersey|Rutgers Cancer Institute of New Jersey|National Cancer Institute (NCI)|AbbVie Prostate Cancer June 2013 Phase 2
NCT00982566 Abbott|Genentech, Inc. Lymphoid Malignancies|Solid Tumors October 2009 Phase 1
NCT01053520 Abbott|Genentech, Inc. Healthy Female Subjects October 2009 Phase 1
NCT00788684 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie CD20-Positive Lymphoid Malignancies|Chronic Lymphoid Leukemia|Hematological Malignancies|Non-Hodgkin's Lymphoma July 28, 2009 Phase 1
NCT01021358 Abbott Lymphoma|Chronic Lymphocytic Leukemia|Solid Tumors January 2010 Phase 1
NCT00887757 Abbott|Genentech, Inc. Solid Tumors September 2009 Phase 1
NCT02591095 Centre Francois Baclesse|ARCAGY/ GINECO GROUP|French Cancer Research Hospital Program Platinum-resistant or Refractory Ovarian Cancer January 2016 Phase 2
NCT00891605 Abbott|Genentech, Inc. Solid Tumors July 2009 Phase 1
NCT00918450 Abbott|Genentech, Inc. B-cell Chronic Lymphocytic Leukemia March 2010 Phase 2
NCT00868413 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Chronic Lymphocytic Leukemia November 2009 Phase 1
NCT00888108 Abbott|Genentech, Inc. Solid Tumor July 2009 Phase 1
NCT00878449 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Solid Tumors October 2009 Phase 1
NCT00406809 AbbVie (prior sponsor, Abbott)|AbbVie Chronic Lymphoid Leukemia|Lymphoid Malignancies|Non-Hodgkin's Lymphoma|Follicular Lymphoma|Mantle Cell Lymphoma|Peripheral T-cell Lymphoma November 2006 Phase 2
NCT00743028 Abbott|Genentech, Inc. Chronic Lymphocytic Leukemia|Lymphomas|Leukemias August 2008 Phase 1
NCT00481091 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Chronic Lymphocytic Leukemia July 25, 2007 Phase 2
NCT00445198 AbbVie (prior sponsor, Abbott)|Genentech, Inc.|AbbVie Small Cell Lung Cancer|Small Cell Lung Carcinoma April 2007 Phase 1|Phase 2
NCT01009073 AbbVie (prior sponsor, Abbott)|AbbVie Solid Tumors October 2009 Phase 1
NCT01087151 Genentech, Inc.|AbbVie (prior sponsor, Abbott) Chronic Lymphocytic Leukemia August 2010 Phase 2
NCT01828476 Rutgers, The State University of New Jersey|Rutgers Cancer Institute of New Jersey|National Cancer Institute (NCI)|AbbVie Prostate Cancer June 2013 Phase 2
NCT00982566 Abbott|Genentech, Inc. Lymphoid Malignancies|Solid Tumors October 2009 Phase 1
NCT01053520 Abbott|Genentech, Inc. Healthy Female Subjects October 2009 Phase 1
NCT01121133 Abbott Lymphoma, Including Chronic Lymphocytic Leukemia|Solid Tumors May 2010 Phase 1
NCT03222609 AbbVie Myelofibrosis (MF) October 2, 2017 Phase 2
NCT03181126 AbbVie Acute Lymphoblastic Leukemia August 25, 2017 Phase 1
NCT01557777 AbbVie (prior sponsor, Abbott)|AbbVie Chronic Lymphocytic Leukemia June 2012 Phase 2
NCT02143401 National Cancer Institute (NCI) Child-Pugh Class A|Child-Pugh Class B|Cirrhosis|Hepatitis B Infection|Hepatitis C Infection|Metastatic Malignant Solid Neoplasm|Recurrent Hepatocellular Carcinoma|Recurrent Malignant Solid Neoplasm|Refractory Malignant Neoplasm|Stage IV Hepatocellular Carcinoma AJCC v7|Unresectable Solid Neoplasm November 7, 2014 Phase 1
NCT02520778 National Cancer Institute (NCI) EGFR Activating Mutation|Recurrent Non-Small Cell Lung Carcinoma|Stage III Non-Small Cell Lung Cancer AJCC v7|Stage IIIA Non-Small Cell Lung Cancer AJCC v7|Stage IIIB Non-Small Cell Lung Cancer AJCC v7|Stage IV Non-Small Cell Lung Cancer AJCC v7 March 31, 2016 Phase 1
NCT02079740 National Cancer Institute (NCI) Advanced Malignant Solid Neoplasm|KRAS Gene Mutation|Metastatic Malignant Solid Neoplasm|NRAS Gene Mutation|Recurrent Colorectal Carcinoma|Recurrent Lung Carcinoma|Recurrent Pancreatic Carcinoma|Stage III Colorectal Cancer AJCC v7|Stage III Lung Cancer AJCC v7|Stage III Pancreatic Cancer AJCC v6 and v7|Stage IIIA Colorectal Cancer AJCC v7|Stage IIIB Colorectal Cancer AJCC v7|Stage IIIC Colorectal Cancer AJCC v7|Stage IV Colorectal Cancer AJCC v7|Stage IV Lung Cancer AJCC v7|Stage IV Pancreatic C March 7, 2014 Phase 1|Phase 2
NCT01989585 National Cancer Institute (NCI) Metastatic Melanoma|Recurrent Melanoma|Solid Neoplasm|Stage IIIA Skin Melanoma|Stage IIIB Skin Melanoma|Stage IIIC Skin Melanoma|Stage IV Skin Melanoma October 25, 2013 Phase 1|Phase 2
NCT01423539 Genentech, Inc.|AbbVie (prior sponsor, Abbott) Diffuse Large B-Cell Lymphoma October 2011 Phase 2
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.0261 mL 5.1303 mL 10.2605 mL
5 mM 0.2052 mL 1.0261 mL 2.0521 mL
10 mM 0.1026 mL 0.5130 mL 1.0261 mL
Kinase Assay
[2]

To measure caspase-3/7 activation, IGROV-1 and SKOV3 cells are seeded in 96-well plates at 5,000 cells per well. After 24 hours, cells are treated with navitoclax (1 μM), paclitaxel (dose range=1-100 nM), or in combination with navitoclax and paclitaxel using the same dosing concentrations. Each treatment is done in duplicate wells. Induction of apoptosis, following treatment at time 0, 4, 24, and 48 hours, is determined using a Caspase-Glo 3/7 assay. A DMSO control is included in all studies. The experiment is conducted twice, and the data are presented as an average of both runs. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

Navitoclax is dissolved in DMSO.

Cells are seeded in 384-well plates at 3,000 cells per well. After 24 hours, cells are treated with navitoclax (dose range of 14 nM-3.3 μM) and paclitaxel (dose range of 15 pM-100 nM) or gemcitabine (dose range of 0.5 nM-3.3 μM) in a 9 by 7 matrix. Each treatment is carried out in quadruplicate. Cells are treated for 72 hours, and cell viability is determined using the CellTiter-Glo assay. Cell viability for each treatment is normalized against the DMSO control group.  MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Navitoclax is administered by oral gavage once daily in a mixture of Phosal 50PG : PEG400 : ethanol.

For systemic Granta 519 tumour models, 2×106 cells are injected via the tail vein in 0.1 mL volume of cell medium on day 0, and treatment is initiated on day 14. All animals are ear-tagged and monitored individually throughout the experiment. Navitoclax is administered by oral gavage once daily in a mixture of Phosal 50PG : PEG400 : ethanol. Bendamustine and rituximab are administered i.v. at 25 and 10 mg/kg, respectively, on day 1. Navitoclax is administered approximately 2 h before bendamustine and rituximab. All trials are comprised of 10 mice per group. Mice are humanely killed when tumours reached a size >2000 mm3 or when any signs of distress are monitored. Signs of distress include loss of ambulation, laboured breathing or weight loss > 20% mean body weight per cage. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
M.Wt

974.61

Formula

C₄₇H₅₅ClF₃N₅O₆S₃

CAS No.

923564-51-6

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

10 mM in DMSO

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

Purity: 99.34%

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Navitoclax
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