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()
    Tipifarnib
    Tipifarnib

    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 #: V0915
    CAS #: 192185-72-1Purity ≥98%

    Description: Tipifarnib (formerly also known as R115777) is a novel, nonpeptidomimetic quinolinone analog, potent and specific farnesyltransferase (FTase) inhibitor with IC50 of 0.6 nM, its anti-proliferative effects are most prominent in H-ras or N-ras mutant cells. Tipifarnib has been investigated in patients 65 years of age and older with newly diagnosed acute myeloid leukemia (AML). It inhibits the Ras kinase in a post translational modification step before the kinase pathway becomes hyperactive. 

    References: Clin Cancer Res. 2012 Feb 15;18(4):1129-37; Cancer Immunol Immunother. 2012 Apr;61(4):523-33. 

    Related CAS: 192185-71-0 (S-Tipifarnib)

    Customer Validation
    Official Supplier of
    • VE
    • OF
    • YALE
    • hhmi
    • 香港大学
    Related Products
    Publications Citing InvivoChem Products
    • Citation of InvivoChem Larotrectinib (V2599) by Cell (2020) 183(5):1202-1218.e25
    • Citation of InvivoChem BMH-21 (V1435) by Cell Stem Cell 2020, 26(6): 845-861.e12.
    • Citation of InvivoChem BMS-582949 (V2668) by Cells 2020, 9(6):1472. doi: 10.3390/cells90614
    • Citation of InvivoChem Resveratrol (V0430) by Arterioscler Thromb Vasc Biol 2020; ATVBAHA12
    • Citation of InvivoChem venetoclax and S63845 (V2797) by Cell Death and Disease (2020) 11:316.
    • Citation of InvivoChem Belumosudil (KD025) by Am J Physiol Renal Physiol. 2019; 317(4):F839-F851.
    • Physicochemical and Storage Information
    • Protocol
    • Quality Control Documentation
    • Related Biological Data
    • Customer Review
    Molecular Weight (MW)489.4
    FormulaC27H22Cl2N4O
    CAS No.192185-72-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 14 mg/mL (28.6 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)15% Captisol+citrate vehicle: 5 mg/mL
    SynonymsR-115777; LX81; Lonafarnib; R115777; R 115777; NSC702818; D03720; trade name Zarnestra


    • 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: Using Tipifarnib 5 μM for 72 hours, the percentage of apoptotic cells is significantly higher in drug-treated compared to DMSO-treated LGL T-cells. Using T-cells from healthy donors, Tipifarnib reduces the percentage of IFNγ-positive cells in a time-dependent manner. Tipifarnib reduces the amount of activated Ras in precipitates compared to DMSO. Tipifarnib exerts selective in vitro toxicity against clonal MDS hematopoiesis at concentrations less than 10 nM the effect being more prominent in white cell progenitors. This action is not due to apoptosis induction as both normal and MDS progenitors displays equivalent DiOC3 and annexin V expression up to 72 hours after exposure to Tipifarnib. Combining Tipifarnib with 10 nM 4-OH-tamoxifen in the presence of E2 reduces the IC50 8-fold from 400 to 50 nM. Tipifarnib induces apoptosis in U937 cells. In addition, Tipifarnib inhibits isolated human farnesyltransferase for a lamin B peptide and for the K-RasB peptide with IC50 of 0.86 nM and 7.9 nM, respectively.


    Kinase Assay: Tipifarnib binds to and inhibits farnesyltransferase (FTase) with IC50 of 0.6 nM.


    Cell Assay: MACS-selected CD34+ cells are seeded in Methocult 4435 'complete' 1% bovine serum albumin, 3 U/mL recombinant human (rh) erythropoietin, 0.1 mM 2-mercaptoethanol, 2 mM L-glutamine and the following cytokines: 50 ng/mL rh stem cell factor, 20 ng/mL rh GM-CSF, 20 ng/mL rh IL-3, 20 ng/mL rh IL-6 and 20 ng/mL h G-CSF. DMSO or Tipifarnib is added at the concentrations of 2.5, 10, 25 and 50 nM at day 1. All cultures are performed in duplicates and the numbers of colonies are scored after 14 days of incubation at 37 °C in a humidified incubator containing 5% CO2.

    In VivoKi-67 is lower in the tumors treated with E2 withdrawal plus R115777 compared with E2 withdrawal alone. The combination of tamoxifen and R115777 results in significantly lower Ki-67 compared with either tamoxifen or R115777 alone (mean of 5% versus 16.9% and 67.3%, respectively). In contrast, no significant difference in apoptotic scores is seen between the treatment groups. R115777 alone also reduces the CTI compared with control. The combination of tamoxifen and R115777 or R115777 coupled with E2 withdrawal is most effective at lowering the CTI (0.8 and 0.7, respectively), which may account for the decrease in tumor volume.
    Animal modelFemale ovariectomized Ncr foxhead nude mice
    Formulation & DosageDissolved in 20% w/v β-cyclodextrin (pH 2.5); 50 mg/kg; Oral gavage  
    ReferencesClin Cancer Res. 2012 Feb 15;18(4):1129-37; Cancer Immunol Immunother. 2012 Apr;61(4):523-33; Mol Cancer Ther. 2007 Sep;6(9):2458-67.


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

    Tipifarnib

    Tipifarnib

    Tipifarnib

    Reduced Th1 cytokine production in LGL leukemia T-cells after tipifarnib treatment. Cancer Immunol Immunother. 2012 Apr;61(4):523-33.

     


    Tipifarnib

    Farnesyltransferase inhibitors reduce IFNγ production in cells from healthy donors. Cancer Immunol Immunother. 2012 Apr;61(4):523-33.

    Tipifarnib

    Deficiency in Th1 differentiation and signaling in FTI-treated cells. Cancer Immunol Immunother.2012 Apr;61(4):523-33. 

    Tipifarnib

    Effect of tipifarnib on chromatin remodeling of the ifng and IL4 genes. Cancer Immunol Immunother. 2012 Apr;61(4):523-33. 


    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?