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ABT-263 (Navitoclax)
Potent Bcl-2 family inhibitor, inhibits Bcl-2, Bcl-xL, and Bcl-w

ABT-263 (Navitoclax)

Catalog No. A3007
Size Price Stock Qty
Evaluation Sample $28.00 In stock
5mg $50.00 In stock
10mg $70.00 In stock
50mg $200.00 In stock
100mg $350.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Jubierre, L., et al. "BRG1/SMARCA4 is essential for neuroblastoma cell viability through modulation of cell death and survival pathways." Oncogene (2016). PMID:26996667

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Chemical structure

ABT-263 (Navitoclax)

Related Biological Data

 ABT-263
ABT-737, or ABT-263 at the indicated doses for 24 hours. Survival data are shown for transitional B cells (n = 3 mice for each genotype) and are the results of 3 independent experiments, each performed in triplicate. Experiments depicted in panels C and D were performed concurrently. Values represent mean ± SEM.

Related Biological Data

 ABT-263
As an inhibitor of Bcl-2, ABT263 is effective to reduce cell viability in HG3-CLL cells. Incubating the cells with ABT263 in 96 well plates (3×104 cells per well) for 24h shows a dose-dependent inhibition of cell viability with EC50 value of 2μM.[Source: Istituto di Scienze dell’ Alimentazione]

Related Biological Data

ABT-263

Biological Activity

ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤1 nM.
Targets Bcl-xL Bcl-2 Bcl-w      
IC50 ≤ 0.5 nM (Ki) ≤1 nM (Ki) ≤ 1 nM (Ki)      

Protocol

Cell experiment:[1]

Cell lines

Murine DO11.10 T-hybridoma cells expressing murine Bcl-2, Bcl-xL and Bcl-w proteins

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reacting condition

None specifc suggestion

Applications

ABT-263 is an antitumor effector in preclinical and early clinical studies. It binds to Bcl-2, Bcl-xL, and Bcl-w in vitro, but only targets Bcl-2 in vivo. In human non-Hodgkin lymphomas, high expression of Bcl-2 sensitized to ABT-263 elevated proapoptotic Bim.

Animal experiment:[2]

Animal models

Immune-deficient NOD/SCID or NOD/SCID, ILγ receptor negative mice

Dosage form

Orally taken at 100 mg/kg/day for 21 days

Application

ABT-263 can largely inhibited the activity of patient-derived pediatric acute lymphoblastic leukemia xenograft. ABT-263 sensitivity was correlated with low MCL1 mRNA expression levels. BH3 profiling revealed that resistance to ABT-263 correlated with mitochondrial priming by NOXA peptide.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

1. Mérino D1, Khaw SL, Glaser SP et al. Bcl-2, Bcl-x(L), and Bcl-w are not equivalent targets of ABT-737 and navitoclax (ABT-263) in lymphoid and leukemic cells.Blood. 2012 Jun 14;119(24):5807-16.

2. Suryani S, Carol H, Chonghaile TN et al. Cell and Molecular Determinants of In Vivo Efficacy of the BH3 Mimetic ABT-263 against Pediatric Acute Lymphoblastic Leukemia Xenografts. Clin Cancer Res. 2014 Jul 10.

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Chemical Properties

Cas No. 923564-51-6 SDF Download SDF
Synonyms Navitoclax,ABT-263,ABT263,ABT 263
Chemical Name 4-[4-[[2-(4-chlorophenyl)-5,5-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide
Canonical SMILES CC1(CCC(=C(C1)CN2CCN(CC2)C3=CC=C(C=C3)C(=O)NS(=O)(=O)C4=CC(=C(C=C4)NC(CCN5CCOCC5)CSC6=CC=CC=C6)S(=O)(=O)C(F)(F)F)C7=CC=C(C=C7)Cl)C
Formula C47H55ClF3N5O6S3 M.Wt 974.61
Solubility Soluble in DMSO > 10 mM Storage Desiccate at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

View Related Products By Research Topics

Research Update

1. The role of lymphatic transport on the systemic bioavailability of the Bcl-2 protein family inhibitors navitoclax (ABT-263) and ABT-199. Drug Metab Dispos. 2014 Feb;42(2):207-12. doi: 10.1124/dmd.113.055053. Epub 2013 Nov 8.
Abstract
ABT-263 tablets (100mg) orally administered to both intact and TDC dogs exhibited low clearance (0.673 ml/min per kilogram) and low volume of distribution (0.5-0.7 l/kg) with a half-life of 22.2 hours and the bioavailablity of 56.5%, where 13.5% of the total ABT-263 dose in TDC dogs was transported in lymph with the bioavailability of 21.7%. However, in fasted TDC dogs, a 1.8-fold decrease in lymph transport of ABT-263 was observed.
2. Navitoclax (ABT-263) and bendamustine ± rituximab induce enhanced killing of non-Hodgkin's lymphoma tumours in vivo. Br J Pharmacol. 2012 Oct;167(4):881-91. doi: 10.1111/j.1476-5381.2012.02048.x.
Abstract
As an inhibitor of Bcl-2, Bcl-x(L) and Bcl-w, ABT-263 exhibits antitumor activity against haematological tumors when used alone or in combination with other agents.
4. Navitoclax (ABT-263) reduces Bcl-x(L)-mediated chemoresistance in ovarian cancer models. Mol Cancer Ther. 2012 Apr;11(4):1026-35. doi: 10.1158/1535-7163.MCT-11-0693. Epub 2012 Feb 1.
Abstract
Synergistic effects against ovarian cancer cells were observed in both ABT-263/paclitaxel and ABT-263/gemcitabine treatments with a stronger effect in ABT-163/paclitaxel treatment killing 50% of tested ovarian cancer cells. The combination of ABT-263 with taxane-based therapy is more suitable for ovarian cancer patients with high levels of Bcl-x(L).
5. Bcl-2, Bcl-x(L), and Bcl-w are not equivalent targets of ABT-737 and navitoclax (ABT-263) in lymphoid and leukemic cells. Blood. 2012 Jun 14;119(24):5807-16. doi: 10.1182/blood-2011-12-400929. Epub 2012 Apr 26.
Abstract
ABT-263, an inhibitor of Bcl-2, Bc,-x(L) and Bcl-w with promising antitumor efficacy, is sensitive to human non-Hodgkin lymphomas with high expression of Bcl-2.

Background

ABT-263 is an orally sellecitive inhibitor of B-cell leukemia 2 (Bcl-2) family of proteins with potential antineoplastic activity. ABT-263 is a small molecular with the formula of C47H55ClF3N5O6S3 and Molecular Weight of 974. As a Bad-like Bh3 minetic, ABT-263 binds to Bcl-2 family proteins Bcl-2, Bcl-xl and Bcl-w, disrupts the interaction between Bcl-2/Bcl-xl /Bcl-w and pro-apoptotic proteins such as Bim, Bad and Bak, which trigger the caspases-initiated cell death pathway to induce apoptosis.

References:

1. Tse et al., ABT-263: A Potent and Orally Bioavailable Bcl-2 Family Inhibitor. Cancer Res. 2008, 68, 3421-3428. 

2. Shoemaker et al., Activity of the Bcl-2 Family Inhibitor ABT-263 in a Panel of Small Cell Lung Cancer Xenograft Models. Clin. Cancer Res. 2008, 14, 3268-3277