Name: ABT-737
Price: 236.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    ABT-737 is a novel and potent inhibitor of B-cell lymphoma 2 (BCL-2) family proteins, which are critical for cell survival and overexpressed in many tumor cells, with high affinity towards BCL-XL, BCL-2, and BCL-w but no affinity towards less homologous proteins, such as BCL-B, MCL-1, and A1. ABT-737 has shown single-agent activity against lymphoma and small-cell lung cancer as well as substantial antimyeloma activity both in vitro and in vivo. In recent studies, acute myeloid leukemia blast, origenitor, and stem cells are effectively killed by ABT-737 with normal hematopoietic cells intact. The disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway could also be induced by ABT-737.
- Properties
  - Alternative Name
    
    ABT 737, ABT737; 4-[4-[[2-(4-chlorophenyl)phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonylbenzamide
    
    CAS Number
    
    852808-04-9
    
    Molecular Formula
    
    C42H45ClN6O5S2
    
    Molecular Weight
    
    813.43
    
    Appearance
    
    A solid
    
    Purity
    
    95.54%
    
    Solubility
    
    ≥40.67 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Kirsteen J. Campbell, Susan M. Mason, et al. "Breast cancer dependence on MCL-1 is due to its canonical anti-apoptotic function." Cell Death Differ. 2021 Sep;28(9):2589-2600. PMID:33785871
    2. Alexander-Floyd J, Haroon S, et al. "Unexpected cell type-dependent effects of autophagy on polyglutamine aggregation revealed by natural genetic variation in C. elegans." BMC Biol. 2020;18(1):18. Published 2020 Feb 24. doi:10.1186/s12915-020-0750-5. PMID:32093691
    3. Lee B, Min JA, et al. "A novel mechanism of irinotecan targeting MDM2 and Bcl-xL." Biochem Biophys Res Commun. 2019 Jun 25;514(2):518-523. PMID:31056264
    4. Thompson PJ, Shah A, et al. "Targeted Elimination of Senescent Beta Cells Prevents Type 1 Diabetes." Cell Metab. 2019 Feb 14. pii: S1550-4131(19)30021-X. PMID:30799288
    5. Rello-Varona S, Fuentes-Guirado M, et al. "Bcl-x(L) inhibition enhances Dinaciclib-induced cell death in soft-tissue sarcomas." Sci Rep. 2019 Mar 7;9(1):3816. PMID:30846724
    6. Yochum ZA, Cades J, et al. "Targeting the EMT transcription factor TWIST1 overcomes resistance to EGFR inhibitors in EGFR-mutant non-small-cell lung cancer." Oncogene. 2018 Aug 31. PMID:30171258
    7. Jeong HJ, Ryu KJ, et al. "Anticancer agent ABT-737 possesses anti-atopic dermatitis activity via blockade of caspase-1 in atopic dermatitis in vitro and in vivo models." Immunopharmacol Immunotoxicol. 2018 Jun 29:1-8. PMID:29957081
    8. Kim HY, Jeong HJ, et al. "Anti-allergic and anti-inflammatory effects of the Bcl-2 inhibitor ABT-737 on experimental allergic rhinitis models." Eur J Pharmacol. 2018 May 30;833:34-43. PMID:29856968
    9. 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
    10. 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
    11. 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
    12. Joel Riley, Giovanni Quarato, et al. "Activated BAX/BAK enable mitochondrial inner membrane permeabilisation and mtDNA release during cell death."bioRxiv. 2018 February 26.
    13. Frevert, Marie Louise. "24 drugs as potential SKP2 Inhibitors: a novel approach to finding new antidepressants. Dissertation, LMU München: Medizinische Fakultät." d-nb.info. 2017.
    14. Xiang XY, Kang JS, et al. "SIRT3 participates in glucose metabolism interruption and apoptosis induced by BH3 mimetic S1 in ovarian cancer cells." Int J Oncol. 2016 Aug;49(2):773-84. PMID:27277143
    15. Kris Cameron Wood,Peter Saville Winter. "Compositions and Methods for Treating Cancer with JAK2 Activity." US Patent App. 15/027,216, 2016.
    16. Moriwaki, Kenta, et al. "The Mitochondrial Phosphatase PGAM5 Is Dispensable for Necroptosis but Promotes Inflammasome Activation in Macrophages." The Journal of Immunology (2015): 1501662. PMID:26582950
    17. Winter PS, et al. "RAS signaling promotes resistance to JAK inhibitors by suppressing BAD-mediated apoptosis." Sci Signal. 2014 Dec 23. PMID:25538080

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