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    Lonafarnib
    Lonafarnib

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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 #: V0916
    CAS #: 193275-84-2Purity ≥98%

    Description: Lonafarnib (formerly also known as SCH66336) is a novel, orally bioavailable and highly potent FPTase (farnesyl protein transferase) inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively. Lonafarnib is also a synthetic tricyclic derivative of carboxamide with antineoplastic properties. Lonarfanib binds to and inhibits farnesyl transferase, an enzyme involved in the post-translational modification and activation of Ras proteins. Ras proteins participate in numerous signalling pathways (proliferation, cytoskeletal organization), and play an important role in oncogenesis. Mutated ras proteins have been found in a wide range of human cancers.

    References: Cancer Res. 1998;58(21):4947-56; Cancer Res. 2003;63(16):4796-800; Cancer Res. 2001;61(11):4425-31.

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    Molecular Weight (MW)638.82
    FormulaC27H31Br2ClN4O2
    CAS No.193275-84-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 127 mg/mL (198.8 mM)
    Water: <1 mg/mL
    Ethanol: 127 mg/mL (198.8 mM)
    SMILESO=C(N1CCC(CC(N2CCC(C3C4=C(Br)C=C(Cl)C=C4CCC5=CC(Br)=CN=C53)CC2)=O)CC1)N
    SynonymsLonafarnib; SCH66336; Trade name: Sarasar; SCH 66336; SCH-66336; 


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    In Vitro

    In vitro activity: SCH66336 at concentration ranging from 0.1 μM to 8 μM suppress growth and induce apoptosis of human head and neck squamous carcinoma cells (HNSCC) in a dose and time dependent manner. SCH66336 (8 μM) suppresses protein kinase B/Akt activity as well as the phosphorylation of the Akt substrates glycogen synthase kinase (GSK)-3β, forkhead transcription factor, and BAD in SqCC/Y1 cells. SCH66336 demonstrate variable antiproliferative effects against the cell lines, with IC50 ranging from 0.6 μM to 32.3 μM. Lonafarnib induces a CCAAT/enhancer-binding protein homologous protein (CHOP)-dependent transactivation of the DR5 promoter, thus induces CHOP-dependent DR5 up-regulation. Lonafarnib (< 10 μM) activates caspase-8 and its downstream caspases, thus induces caspase-8-dependent apoptosis in H1792 cells. Lonafarnib (5 μM) up-regulate DR5 expression, increase cell-surface DR5 distribution, and enhance tumor necrosis factor-related apoptosis-inducing ligand-induced apoptosis in H1792 cells.


    Kinase Assay: FPTactivity is determined by measuring the transfer of [3H]farnesyl from [3H]farnesyl PPi to trichloroacetic acid-precipitable Ha-Ras-CVLS. GGPT-1 activity is similarly determined using [3H]geranylgeranyl diphosphate and Ha-Ras-CVLL as substrates.


    Cell Assay: The cells are seeded in 96-well cell-culture cluster plates at a density that allowed control cultures to grow exponentially for 5 days. After 24 hours, the cells are treated with different concentrations of SCH66336. SCH66336 is dissolved in DMSO. Control cultures received the same amount of DMSO as the treated cultures do. Cell numbers are estimated after 5 days of treatment by SRB assay. The percentage of growth inhibition is calculated by using the equation: percentage growth inhibition = (1 − At/Ac) × 100, where At and Ac represent the absorbance in treated and control cultures, respectively. The drug concentration causing a 50% cell growth inhibition (IC50), is determined by interpolation from dose-response curves.

    In VivoSCH66336 inhibits HTBI77 human lung carcinoma xenograft growth in nude mice in a dose-dependent fashion. SCH66336 dosed at 50 mg/kg p.o. bid by oral gavage inhibits tumor growth with up to 69% growth inhibition after 21 days of treatment in NOD/SCID mice bearing s.c. flank XEN01, XEN05 or XEN08 GBM xenografts.
    Animal modelNOD/SCID mice between 6–12 weeks of age
    Formulation & DosageDissolved in 20% (w/v) HPβCD; 50 mg/kg; Oral gavage  
    ReferencesCancer Res. 1998 Nov 1;58(21):4947-56; Cancer Res. 2003 Aug 15;63(16):4796-800; Cancer Res. 2001 Jun 1;61(11):4425-31.


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

    Lonafarnib

    Effects of SCH66336 on the cell growth and colony formation in SqCC/Y1 cells. Cancer Res. 2003 Aug 15;63(16):4796-800.
     

    Lonafarnib

    Effects of SCH66336 on apoptosis induction in SqCC/Y1 cells. Cancer Res. 2003 Aug 15;63(16):4796-800.
     

    Lonafarnib

    Phosphorylation level and protein expression changes by SCH66336 in SqCC/Y1 cells. Cancer Res. 2003 Aug 15;63(16):4796-800.


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