My cart
In the shopping cart is not goods, to choose and buy!
  • Product Name
  • Size
  • Quantity
  • Amount
    Selected items : 0 pieces Total : CHECK OUT()
    3-deazaneplanocin A (DZNeP; NSC 617989) HCl
    3-deazaneplanocin A (DZNeP; NSC 617989) HCl

    Price:
    Market Price:

    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V0384
    CAS #: 120964-45-6Purity ≥98%

    Description: 3-deazaneplanocin A (known also as DZNep; NSC-617989), an adenosine analog, is a novel and competitive inhibitor of S-adenosylhomocysteine hydrolase and an EZH2 (histone methyltransferase ) inhibitor with anticancer activity. It inhibits S-adenosylhomocysteine hydrolase with a Ki of 50 pM in a cell-free assay. 3-deazaneplanocin A demostrates excellent antiproliferative activity and high in vivo antitumor efficacy. It disrupts polycomb-repressive complex 2 (PRC2), and induces apoptosis, while inhibiting proliferation and metastasis, in cancer cells, including acute myeloid leukemia, breast cancer and glioblastoma. DZNep is a promising therapeutic agent for ovarian cancer cells, with potential to inhibit proliferation, induce apoptosis and decrease migration. 

    References:Blood. 2009 Sep 24;114(13):2733-43; J Med Chem. 1989 Jul;32(7):1442-6.

    Related CAS #: 120964-45-6 (HCl); 102052-95-9 (free base);     

    Customer Validation
    Official Supplier of
    • VE
    • OF
    • YALE
    • hhmi
    • 香港大学
    Related Products
    Publications Citing InvivoChem Products
    • Physicochemical and Storage Information
    • Protocol
    • Quality Control Documentation
    • Related Biological Data
    • Customer Review
    Molecular Weight (MW)298.73
    FormulaC12H14N4O3.HCl
    CAS No.120964-45-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 52 mg/mL (174.1 mM)
    Water: 52 mg/mL (174.1 mM)
    Ethanol: <1 mg/mL
    Other info
    Chemical Name: (1S,2R,5R)-5-(4-amino-1H-imidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol hydrochloride
    InChi Key: UNSKMHKAFPRFTI-FDKLLANESA-N
    InChi Code: InChI=1S/C12H14N4O3.ClH/c13-12-9-7(1-2-14-12)16(5-15-9)8-3-6(4-17)10(18)11(8)19;/h1-3,5,8,10-11,17-19H,4H2,(H2,13,14);1H/t8-,10-,11+;/m1./s1
    SMILES Code: O[[email protected]@H]1[[email protected]](O)C(CO)=C[[email protected]]1N2C=NC3=C2C=CN=C3N.[H]Cl 
    SynonymsNSC 617989 HCl;  NSC-617989 HCl; 3-deazaneplanocin A HCl; 3-deazaneplanocin A hydrochloride; DZNep; NSC617989; 


    • Molarity Calculator
    • Dilution Calculator
    • The molarity calculator equation

      Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

      • Mass
      • Concentration
      • Volume
      • Molecular Weight *
      • =
      • ×
      • ×
    • The dilution calculator equation

      Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

      This equation is commonly abbreviated as: C1V1 = C2V2

      • Concentration (start)
      • ×
      • Volume (start)
      • =
      • Concentration (final)
      • ×
      • Volume (final)
      • ×
      • =
      • ×
      • C1
      •  
      • V1
      •  
      • C2
      •  
      • V2
    In Vitro

    In vitro activity: 3-Deazaneplanocin A (DZNep) hydrochloride causes dose-dependent inhibition of cell proliferation of NSCLC cell lines, and the IC0 values range from 0.08 to 0.24 μM

    In VivoThe survival of NOD/SCID mice with acute myeloid leukemia (AML) due to HL-60 cells is significantly higher, if treated with 3-Deazaneplanocin A (DZNep) and LBH589 (PS) compare to treatment with PS, 3-Deazaneplanocin A, or vehicle alone (P<0.05). Median survival is as follows: control, 36 days; PS, 42 days; 3-Deazaneplanocin A, 43 days; and 3-Deazaneplanocin A plus PS, 52 days
    Animal modelNOD/SCID mice
    Formulation & DosageMice: HL-60 cells (5 million) are injected into the tail vein of female nonobese diabetic/severe combined immunodeficiency (NOD/SCID) mice, and the mice are monitored for 7 days. The following treatments are administered in cohorts of 7 mice for each treatment: vehicle alone, 1 mg/kg 3-Deazaneplanocin A, 10 mg/kg PS, and 3-Deazaneplanocin A plus PS. Treatments are initiated on day 7. 3-Deazaneplanocin A is administered twice per week (Tuesday-Thursday) intraperitoneally for 2 weeks, and then discontinued. PS is administered 3 days per week (Monday, Wednesday, and Friday) for 4 weeks. The survival of mice from the tail vein model is represented with a Kaplan-Meier survival plot.


    Rats: Male wistar rats are used. The acute toxicity study is carried out to determine the NOAEL of 3-Deazaneplanocin A in rats. In total, 20 rats are divided into 4 groups of five each. Three groups are intravenously administered 20, 15, 10 mg/kg body weight (BW) DZNep solution by the tail vein. The remaining group is given physiological saline (0.9% NaCl saline) as the control group. Then, the NOAEL of free DZNep is determined, depending on the following endpoint parameters obtained.

    ReferencesBlood, 2009, 114(13), 2733-2743.Mol Cancer Ther. 2012 Aug;11(8):1735-46.


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

    3-deazaneplanocin A (DZNeP) HCl

    SGC707 binds to PRMT3 in cells and reduces PRMT3-dependent H4R3me2a. Angew Chem Int Ed Engl. 2015 Apr 20; 54(17): 5166–5170.



    评论

      Home Prev Next Last page / pices

      发评论

      ×
      Your information is safe with us. * Required Fields.
      Products are for research use only;  We do not sell to patients
      Tel: 1-708-310-1919
      Fax: 1-708-557-7486
      Subscribe to our E-newsletter
      • Name*
      • *
      • E-mail*
      • *
      • instructions:
      • *
      Copyright 2020 InvivoChem LLC | All Rights Reserved
      prompt
      Do you confirm the receipt?