Name: ABT-263 (Navitoclax)
Price: 260.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    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.
    
    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
- Properties
  - Alternative Name
    
    Navitoclax,ABT-263,ABT263,ABT 263; (R)-4-(4-((4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((4-((4-morpholino-1-(phenylthio)butan-2-yl)amino)-3-((trifluoromethyl)sulfonyl)phenyl)sulfonyl)benzamide
    
    CAS Number
    
    923564-51-6
    
    Molecular Formula
    
    C47H55ClF3N5O6S3
    
    Molecular Weight
    
    974.61
    
    Purity
    
    99.02%
    
    Solubility
    
    ≥48.73 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
    
    Storage
    
    Desiccate at -20°C
    
    * For Research Use Only
- Reference
  - 1. Amani A. Gillette, Rebecca A. DeStefanis, et al. "Inhibition of B-cell lymphoma 2 family proteins alters optical redox ratio, mitochondrial polarization, and cell energetics independent of cell state." J Biomed Opt. 2022 May;27(5):056505. PMID: 35643815
    2. Magdalena Delgado, Randall R. Rainwater, et al. "Primary acute lymphoblastic leukemia cells are susceptible to microtubule depolymerization in G1 and M phases through distinct cell death pathways." J Biol Chem. 2022 Jun;298(6):101939. PMID: 35436470
    3. Gabriele Manzella, Devmini C Moonamale, et al. "A combinatorial drug screen in PDX-derived primary rhabdomyosarcoma cells identifies the NOXA - BCL-XL/MCL-1 balance as target for re-sensitization to first-line therapy in recurrent tumors." Neoplasia. 2021 Sep;23(9):929-938. PMID: 34329950
    4. Hae Rim Jung, Yumi Oh, et al. "CRISPR screens identify a novel combination treatment targeting BCL-X L and WNT signaling for KRAS/BRAF-mutated colorectal cancers." Oncogene. 2021 May;40(18):3287-3302. PMID: 33846570
    5. Melod Mehdipour, Taha Mehdipour, et al. "Plasma dilution improves cognition and attenuates neuroinflammation in old mice." Geroscience. 2020 Nov 15. PMID: 33191466
    6. Mariana Boroni, Alessandra Zonari, et al. "Highly accurate skin-specific methylome analysis algorithm as a platform to screen and validate therapeutics for healthy aging." Clinical Epigenetics volume 12, Article number: 105 (2020);13 July 2020. PMID: 32660606
    7. Nicolas Malaquin, Arthur Vancayseele, et al. "DNA Damage- But Not Enzalutamide-Induced Senescence in Prostate Cancer Promotes Senolytic Bcl-xL Inhibitor Sensitivity." Cells 2020, 9(7), 1593;1 July 2020. PMID: 32630281
    8. Lee YC, Shi YJ, et al. "GSK3β suppression inhibits MCL1 protein synthesis in human acute myeloid leukemia cells." J Cell Physiol. 2020;10.1002/jcp.29884. PMID: 32572959
    9. Wang LJ, Liou LR, et al. "Albendazole-Induced SIRT3 Upregulation Protects Human Leukemia K562 Cells from the Cytotoxicity of MCL1 Suppression." Int J Mol Sci. 2020;21(11):3907. PMID: 32486166
    10. Shahbandi A, Rao SG, et al. "BH3 mimetics selectively eliminate chemotherapy-induced senescent cells and improve response in TP53 wild-type breast cancer." Cell Death Differ. 2020;10.1038/s41418-020-0564-6. PMID: 32457483
    11. Lee YC, Wang LJ, et al. "Inhibition of EGFR pathway promotes the cytotoxicity of ABT-263 in human leukemia K562 cells by blocking MCL1 upregulation." Biochem Pharmacol. 2020;178:114047. PMID: 32446890
    12. Parrilla A, Barber M, et al. "Aurora Borealis (Bora), Which Promotes Plk1 Activation by Aurora A, Has an Oncogenic Role in Ovarian Cancer." Cancers (Basel). 2020;12(4):886. PMID: 32268485
    13. Hee Yeon Kim, Byung Il Lee, et al. "Gossypol Suppresses Growth of Temozolomide-Resistant Glioblastoma Tumor Spheres." Biomolecules 2019, 9(10), 595.
    14. Villalobos-Ortiz M, Ryan J, et al. "BH3 profiling discriminates on-target small molecule BH3 mimetics from putative mimetics." Cell Death Differ. 2019 Jul 22. PMID: 31332296
    15. Britt EL, Raman S, et al. "Combination of fenretinide and ABT-263 induces apoptosis through NOXA for head and neck squamous cell carcinoma treatment." PLoS One. 2019 Jul 5;14(7):e0219398. PMID: 31276572
    16. Santos LC, Vogel R, et al. "Mitochondrial origins of fractional control in regulated cell death." Nat Commun. 2019 Mar 21;10(1):1313. PMID: 30899020
    17. Joe T Sharick, Christine M Walsh, et al. "Optical Metabolic Imaging of Heterogeneous Drug Response in Pancreatic Cancer Patient Organoids." bioRxiv. 2019 February 06.
    18. Wu S, Fatkhutdinov N, et al. "SWI/SNF catalytic subunits' switch drives resistance to EZH2 inhibitors in ARID1A-mutated cells." Nat Commun. 2018 Oct 8;9(1):4116. PMID: 30297712
    19. Bera R, Chiu MC, et al. "Genetic and Epigenetic Perturbations by DNMT3A-R882 Mutants Impaired Apoptosis through Augmentation of PRDX2 in Myeloid Leukemia Cells." Neoplasia. 2018 Nov;20(11):1106-1120. PMID: 30245403
    20. Roscoe I, Parker M, et al. "Human Serum Albumin and the p53-Derived Peptide Fusion Protein Promotes Cytotoxicity Irrespective of p53 Status in Cancer Cells." Mol Pharm. 2018 Oct 10. PMID: 30226785
    21. Delgado M, Chambers TC. "Microtubules play an essential role in the survival of primary acute lymphoblastic leukemia cells advancing through G1 phase." Cell Cycle. 2018;17(14):1784-1796. PMID: 29995568
    22. Lee YC, Wang LJ, et al. "ABT-263-induced MCL1 upregulation depends on autophagy-mediated 4EBP1 downregulation in human leukemia cells." Cancer Lett. 2018 Jun 15;432:191-204. PMID: 29913235
    23. Cao Y, Chen M, et al. "The proton pump inhibitor pantoprazole disrupts protein degradation systems and sensitizes cancer cells to death under various stresses."Cell Death Dis. 2018 May 22;9(6):604. PMID: 29789637
    24. Giampazolias E, Zunino B, et al. "Mitochondrial permeabilization engages NF-κB-dependent anti-tumour activity under caspase deficiency." Nat Cell Biol. 2017 Sep;19(9):1116-1129. PMID: 28846096
    25. Russo M, Milito A, et al. "CK2 and PI3K are direct molecular targets of quercetin in chronic lymphocytic leukaemia." Oncotarget. 2017 Jun 27;8(26):42571-42587. PMID: 28489572
    26. Luis C Santos, Robert Vogel, et al. "Origins of fractional control in regulated cell death" bioRxiv.Oct. 10, 2017.
    27. Jubierre Zapater, Luz. "Epigenetic regulators in neuroblastoma: BRG1, a future therapeutic target." tdx.cat.2017-10-09.
    28. Panayotopoulou EG, Müller AK, et al. "Targeting of apoptotic pathways by SMAC or BH3 mimetics distinctly sensitizes paclitaxel-resistant triple negative breast cancer cells."Oncotarget. 2017 Jul 11;8(28):45088-45104. PMID: 28187446
    29. Olson OC, Kim H, et al. "Tumor-Associated Macrophages Suppress the Cytotoxic Activity of Antimitotic Agents." Cell Rep. 2017 Apr 4;19(1):101-113. PMID: 28380350
    30. Jubierre, L., et al. "BRG1/SMARCA4 is essential for neuroblastoma cell viability through modulation of cell death and survival pathways." Oncogene (2016). PMID: 26996667