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()
    Tanzisertib (CC-930)
    Tanzisertib (CC-930)

    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 #: V1565
    CAS #: 899805-25-5 Purity ≥98%

    Description: Tanzisertib (formerly known as CC-930, JNK-930, JNKI-1, CC 930) is a potent, specific and and orally bioavailable JNK1/JNK2/JNK3 inhibitor that has the potential to be used for the treatment of fibrotic and infammatory indications. Tanzisertib is in Phase 1 clinical trial and may have potential use for prevention and treatment of dermal fibrosis. CC-930 is kinetically competitive with ATP in the JNK-dependent phosphorylation of the protein substrate c-Jun and potent against all isoforms of JNK [Ki(JNK1) = 44 ± 3 nM, IC50(JNK1) = 61 nM, Ki(JNK2) = 6.2 ± 0.6 nM, IC50(JNK2) = 5 nM, IC50(JNK3) = 5 nM] and selective against MAP kinases ERK1 and p38a with IC50 of 0.48 and 3.4 μM respectively. 

    References: Bioorg Med Chem Lett. 2012;22(3):1433-8; J Hepatol. 2014 Dec;61(6):1376-84; Ann Rheum Dis. 2012;71(5):737-45.

    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)448.44
    FormulaC21H23F3N6O2
    CAS No.899805-25-5 (free base);
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 10 mM
    Water: <1 mg/mL
    Ethanol: N/A
    SMILES CodeO[[email protected]]1CC[[email protected]](NC2=NC=C3N=C(NC4=C(F)C=C(F)C=C4F)N([[email protected]@H]5COCC5)C3=N2)CC1
    SynonymsCC930, JNK-930, JNKI-1, CC 930, Tanzisertib, JNK930, JNKI1, CC-930, JNK 930, JNKI 1


    • 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: Tanzisertib (also known as CC-930) is a potent, specific and and orally bioavailable JNK1/JNK2/JNK3 inhibitor that has the potential to be used for the treatment of fibrotic and infammatory indications.Tanzisertib is in Phase 1 clinical trial and may have potential use for prevention and treatment of dermal fibrosis. CC-930 inhibits the formation of phospho-cJun in human PBMC stimulated by phorbol-12-myristate-13-acetate and phytohemeagglutinin (IC50=1 μM). CC-930 (1-2 μM) substantially reduces hepatocyte apoptosis and necrosis, abrogates apoptosis and necrosis in FC-loaded WT hepatocytes. CC-930 blocks the JNK pathway that is activated by pro-fibrotic cytokines in systemic sclerosis.


    Kinase Assay:  CC-930 is kinetically competitive with ATP in the JNK-dependent phosphorylation of the protein substrate c-Jun and potent against all isoforms of JNK [Ki(JNK1) = 44 ± 3 nM, IC50(JNK1) = 61 nM, Ki(JNK2) = 6.2 ± 0.6 nM, IC50(JNK2) = 5 nM, IC50(JNK3) = 5 nM] and selective against MAP kinases ERK1 and p38a with IC50 of 0.48 and 3.4 μM respectively. 


    Cell Assay: Systemic sclerosis (SSc) fibroblasts are incubated with 1 µM CC-930 in 96-well plates for 20 h. Then MTT is added at a final concentration of 1 mg/mL, and the cells are further incubated at 37°C for 4 h. Mock-treated fibroblasts are used as controls, and all other results are normalised to untreated cells.

    In VivoIn the acute rat LPS-induced TNFα production PK-PD model, the compound inhibits the production of TNFα by 23% and 77% at 10 and 30 mg/kg oral dose respectively. CC-930 is well-tolerated and exposure is dose-proportional.  
    Animal modelMale C57Bl/6 mice  
    Formulation & DosageDissolved in 5% DMA and 30% PEG 400 (i.v.) or 0.5% CMC/0.25% Tween80(p.o.); 2 mg/kg(i.v.) or 10 mg/kg(p.o.); i.v. or p.o.
    ReferencesBioorg Med Chem Lett. 2012;22(3):1433-8; J Hepatol. 2014 Dec;61(6):1376-84; Ann Rheum Dis. 2012;71(5):737-45.


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

    14Crystal structure of 1 in JNK3 active site.15

    Bioorg Med Chem Lett. 2012 Feb 1;22(3):1433-8.
     

    Compound 1 docked in the p38α active site.16

    Bioorg Med Chem Lett. 2012 Feb 1;22(3):1433-8.


    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?