ABT-199 (Venetoclax), Bcl-2 inhibitor. (ab217298)

Overview

  • Product name
    ABT-199 (Venetoclax), Bcl-2 inhibitor.
  • Description
    Potent, selective Bcl-2 inhibitor.
  • Alternative names
    • 4-[4-[[2-(4-Chlorophenyl)-4,4-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]-N-[[3-nitro-4-[[(tetrahydro-2H-pyran-4-yl)methyl]amino]phenyl]sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide
    • GDC-0199
    • Venetoclax
  • Biological description

    Potent, selective Bcl-2 inhibitor (Ki <0.01 nM) that inhibits the growth of Bcl-2–dependent tumors while sparing platelets. Bcl-2–specific BH3 mimetic. Promising agent in the treatment of chronic lymphocytic leukaemic and estrogen receptor-positive breast cancer.


     

  • Purity
    > 98%
  • CAS Number
    1257044-40-8
  • Chemical structure
    Chemical Structure

Properties

  • Selectivity

    Bcl-2

  • Chemical name
    2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4’-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1’-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((3-nitro-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)phenyl)sulfonyl)benzamide
  • Molecular weight
    868.44
  • Molecular formula
    C45H50ClN7O7S
  • PubChem identifier
    49846579
  • Storage instructions
    Shipped at 4°C. Store at -20°C. Store under desiccating conditions.
  • Solubility overview
    Soluble in DMSO to 50 mM
  • SMILES
    CC1(CCC(=C(C1)C2=CC=C(C=C2)Cl)CN3CCN(CC3)C4=CC(=C(C=C4)C(=O)NS(=O)(=O)C5=CC(=C(C=C5)NCC6CCOCC6)[N+](=O)[O-])OC7=CN=C8C(=C7)C=CN8)C
  • Source

    Synthetic

References

This product has been referenced in:
  • Itchaki G & Brown JR The potential of venetoclax (ABT-199) in chronic lymphocytic leukemia. Ther Adv Hematol 7:270-287 (2016). Read more (PubMed: 27695617) »
  • Zhao J  et al. Inhibition of CHK1 enhances cell death induced by the Bcl-2-selective inhibitor ABT-199 in acute myeloid leukemia cells. Oncotarget 7:34785-99 (2016). Read more (PubMed: 27166183) »
  • Souers AJ  et al. ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat Med 19:202-8 (2013). Read more (PubMed: 23291630) »
  • Vandenberg CJ & Cory S ABT-199, a new Bcl-2-specific BH3 mimetic, has in vivo efficacy against aggressive Myc-driven mouse lymphomas without provoking thrombocytopenia. Blood 121:2285-8 (2013). Read more (PubMed: 23341542) »
  • Davids MS & Letai A ABT-199: taking dead aim at BCL-2. Cancer Cell 23:139-41 (2013). Read more (PubMed: 23410971) »

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Please note: All products are "FOR RESEARCH USE ONLY AND ARE NOT INTENDED FOR DIAGNOSTIC OR THERAPEUTIC USE, NOT FOR USE IN HUMANS"

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