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      ABT-737
      ABT-737

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      This product is for research use only, not for human use. We do not sell to patients.
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      InvivoChem Cat #: V0002
      CAS #: 852808-04-9Purity ≥98%

      Description: ABT-737 is a novel, potent,  selective and orally available BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in enzymatic assays, respectively. It does not inhibit Mcl-1, Bcl-B or Bfl-1 etc. It is currently in Phase 2 clinical trial for cancer treatment. 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. The mechanism of action of ABT-737 is to mimic BH3 (the native ligand of BCL-2) and act as a BCL-2 inhibitor. It blocks the anti-apoptotic BCL-2 protein, leading to programmed cell death of CLL cells.

      References: Cancer Res. 2007 Feb 1;67(3):1176-83.; Cell Death Differ. 2013 Jan;20(1):57-63. 

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      Molecular Weight (MW)813.43
      FormulaC42H45ClN6O5S2
      CAS No.852808-04-9
      Storage-20℃ for 3 years in powder form
      -80℃ for 2 years in solvent
      Solubility (In vitro)DMSO:    100 mg/mL (122.93 mM)
      Water:     <1 mg/mL (slightly soluble or insoluble)
      Ethanol:  <1 mg/mL
      Solubility (In vivo)30% Propylene glycol, 5% Tween 80, 65% D5W: 30mg/mL
      SMILES CodeO=C(NS(=O)(C1=CC=C(N[[email protected]](CCN(C)C)CSC2=CC=CC=C2)C([N+]([O-])=O)=C1)=O) C3=CC=C(N4CCN(CC5=CC=CC=C5C6=CC=C(Cl)C=C6) CC4)C=C3
      Chemical Name(R)-4-(4-((4'-chloro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((4-((4-(dimethylamino)-1-(phenylthio)butan-2-yl)amino)-3-nitrophenyl)sulfonyl)benzamide
      SynonymsABT 737; ABT-737; ABT737


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      GeneralIn aggressive leukemia model, ABT-737 suppresses the leukemia burden by 53% at 30 mg/kg and extended survival of mice.
      Animal modelScid mice injected with Luc-expressing FD/ΔRaf-1:ER cells
      Formulation1 g/mL stock solution of ABT-737 in DMSO is added to a mixture of 30% propylene glycol, 5% Tween 80, 65% D5W (5% dextrose in water) (pH 4−5; final concentration of DMSO ≤ 1%)
      Dosages20 and 30 mg/kg
      AdministrationFor intraperitoneal (i.p.) every day
      References 2006 Nov;10(5):375-88.

      These protocols are for reference only. InvivoChem does not independently validate these methods.

      ABT-737

      Whole cell lysates of Mel-RM and MM200 cells were subjected to Western blot analysis following treatment with ABT-737 (10µM) for indicated periods. Data are representative of three individual experiments.

      ABT-737

      As an inhibitor of Bcl-2, ABT-737 is effective to reduce cell viability in HG3-CLL cells. Incubating the cells with ABT-737 in 96 well plates (3×104 cells per well) for 24h shows a dose-dependent inhibition of cell viability with EC50 value of 500nM.

      ABT-737

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