Navitoclax (ABT-263)

Alias: Navitoclax; ABT 263; ABT-263; ABT263
Cat No.:V0003 Purity: ≥98%
Navitoclax (formerly ABT-263) is a novel, highly potent,orally bioavailable small-molecule inhibitor of the BCL (B-cell leukemia) protein family such as Bcl-xL, Bcl-2 and Bcl-w with Ki of ~ 0.5 nM, ~1 nM and ~1 nM in cell-free assays.
Navitoclax (ABT-263) Chemical Structure CAS No.: 923564-51-6
Product category: Bcl-2
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of Navitoclax (ABT-263):

  • Navitoclax-d8 (rooting powder 263 d8)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Purity: =100%

Product Description

Navitoclax (formerly ABT-263) is a novel, highly potent, orally bioavailable small molecule inhibitor of the BCL (B-cell leukemia) protein family with Ki of 0.5 nM, 1 nM, and 1 nM in cell-free assays. The BCL (B-cell leukemia) protein family includes Bcl-xL, Bcl-2, and Bcl-w. It is currently undergoing Phase studies for the treatment of both solid and liquid tumors and has the potential to fight cancer. ABT-263 mimicks the Bad-like BH3 and binds to Bcl-2 family proteins Bcl-2, Bcl-xl and Bcl-w which disrupts the interaction between Bcl-2/Bcl-xl /Bcl-w and pro-apoptotic proteins such as Bim(Bcl-2-interacting mediator of cell death), Bad (Bcl-2-associated death promoter) and Bak(BCL2-antagonist/killer 1), eventually it will trigger the caspases-initiated cell death pathway to induce apoptosis.

Biological Activity I Assay Protocols (From Reference)
Bcl-W (Ki=1 nM); Bcl-xL (Ki=1 nM); Bcl-2 (Ki=1 nM)
ln Vitro
The Bcl-2/Bcl-xL interactions with pro-apoptotic proteins are disrupted by ABT-263, which is structurally related to ABT-737. The maintenance, progression, and chemoresistance of tumors are frequently linked to overexpression of prosurvival Bcl-2 family members. ABT-263 exhibits the defense provided by overexpression of Bcl-2 or Bcl-xL with EC50 values of 60 nM and 20 nM, respectively. ABT-263 inhibits 50% of growth in the most sensitive line (H146) with an EC50 of 110 nM, whereas the least sensitive line (H82) exhibits a wide range of cellular activity with an EC50 of 22 M. The two most resistant cell lines (H1048 and H82) are also similarly resistant to ABT-263, as are all four cell lines (H146, H889, H1963, and H1417) with EC50 values of less than 400 nM.
ln Vivo
In the H345 xenograft model, significant antitumor efficacy is seen with 80% TGI and 20% of treated tumors indicating at least a 50% reduction in tumor volume. In xenograft models of small-cell lung cancer and acute lymphoblastic leukemia, oral administration of ABT-263 alone results in total tumor regressions. ABT-263 significantly improves the efficacy of clinically pertinent therapeutic regimens in xenograft models of aggressive B-cell lymphoma and multiple myeloma, where it exhibits modest or no single agent activity.
Enzyme Assay
Binding affinities (Ki or IC50) of ABT-263 against different isoforms of Bcl-2 family are determined with competitive fluorescence polarization assays. The following peptide probe/protein pairs are used: f-bad (1 nM) and Bcl-xL (6 nM), f-Bax (1 nM) and Bcl-2 (10 nM), f-Bax (1 nM) and Bcl-w (40 nM), f-Noxa (2 nM) and Mcl-1 (40 nM), and f-Bax (1 nM) and Bcl-2-A1 (15 nM). Binding affinities for Bcl-xL are also determined using a time-resolved fluorescence resonance energy transfer assay. Bcl-xL (1 nM, His tagged) is mixed with 200 nM f-Bak, 1 nM Tb-labeled anti-His antibody, and ABT-263 at room temperature for 30 min. Fluorescence is measured on an Envision plate reader using a 340/35 nm excitation filter and 520/525 (f-Bak) and 495/510 nm (Tb-labeled anti-His antibody) emission filters.
Cell Assay
Human tumor cell lines SCLC cell lines are maintained at 37℃ containing 5% CO2. SCLC cell lines are cultured in RPMI 1640 with 10% fetal bovine serum (FBS), 1% sodium pyruvate, 25 mM HEPES, 4.5 g/L glucose, and 1% penicillin/streptomycin. Leukemia and lymphoma cell lines are cultured in RPMI 1640 supplemented with 10% FBS and 1% penicillin/streptomycin. Cells (1-5×10 4) are treated by ABT-263 for 48 hours in 96-well culture plates in a final volume of 100 μL and cytotoxicity is assessed with the CellTiter Glo assay. In vitro cyto toxicity of ABT-263 is assayed.
Animal Protocol
100 mg/kg/day
Formulated in 10% ethanol, 30% polyethylene glycol 400, and 60% Phosal 50 PG
C.B -17 scid-bg or C.B -17 scid mice

[1]. Initial testing (stage 1) of the BH3 mimetic ABT-263 by the pediatric preclinical testing program. Pediatr Blood Cancer. 2008 Jun;50(6):1181-1189.

[2]. Navitoclax (ABT-263) reduces Bcl-x(L)-mediated chemoresistance in ovarian cancer models.Mol Cancer Ther. 2012 Apr;11(4):1026-1035.

[3]. The Bcl-2/Bcl-X(L)/Bcl-w inhibitor, navitoclax, enhances the activity of chemotherapeutic agents in vitro and in vivo. Mol Cancer Ther. 2011 Dec;10(12):2340-9.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
Molecular Weight
Exact Mass
Elemental Analysis
C, 57.92; H, 5.69; Cl, 3.64; F, 5.85; N, 7.19; O, 9.85; S, 9.87
Related CAS #
Solid powder
InChi Key
InChi Code
Chemical Name
Navitoclax; ABT 263; ABT-263; ABT263
HS Tariff Code

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO:~100 mg/mL (~102.6 mM)
Water: <1 mg/mL(slightly soluble or insoluble)
Ethanol: <1 mg/mL
Solubility (In Vivo)
55% DMSO+Corn oil: 8mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.


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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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Clinical Trial Information
NCT Number Status Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04472598 Active
Drug: Navitoclax
Drug: Ruxolitinib
Drug: Placebo for Navitoclax
Myelofibrosis (MF) AbbVie September 29, 2020 Phase 3
NCT03222609 Active
Drug: Ruxolitinib
Drug: Navitoclax
Myelofibrosis (MF) AbbVie October 31, 2017 Phase 2
NCT02520778 Active
Drug: Navitoclax
Drug: Osimertinib
Stage III Lung Non-Small
Cell Cancer AJCC v7
National Cancer Institute
August 30, 2016 Phase 1
NCT04041050 Active
Drug: Navitoclax
Drug: Ruxolitinib
Drug: Celecoxib
Myeloproliferative Neoplasm AbbVie November 8, 2019 Phase 1
NCT02143401 Active
Drug: Sorafenib
Drug: Sorafenib Tosylate
Hepatitis B Infection
National Cancer Institute
November 7, 2014 Phase 1
Biological Data
  • ABT-263 (Navitoclax)

    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.
  • ABT-263 (Navitoclax)

  • ABT-263 (Navitoclax)

    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.
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