1. Apoptosis
  2. Bcl-2 Family

Navitoclax (Synonyms: ABT-263; ABT 263; ABT263)

Cat. No.: HY-10087 Purity: 99.34%
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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10 mM * 1 mL in DMSO $86 In-stock
5 mg $50 In-stock
10 mg $80 In-stock
25 mg $140 In-stock
50 mg $200 In-stock
100 mg $350 In-stock
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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].

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.

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. 

Animal Administration
[3]

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.

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

Purity: 99.34%

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Navitoclax
Cat. No.:
HY-10087
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