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    LB42708
    LB42708

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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 #: V0921
    CAS #: 226929-39-1Purity ≥98%

    Description: LB42708 is a novel, potent, and orally bioactive, nonpeptidic farnesyltransferase (FTase) inhibitor with IC50 of 0.8, 1.2, and 2.0 nM toward H-ras, N-ras, and K-ras, respectively. LB42708 inhibited VEGF-induced Ras activation and subsequently suppressed angiogenesis in vitro and in vivo by blocking the MAPK and PI3K/Akt/endothelial nitric-oxide synthase pathways in endothelial cells without altering FAK/Src activation. 

    References: J Immunol. 2004 Jul 15;173(2):1276-83; Toxicol Appl Pharmacol. 2006 Sep 15;215(3):317-29; Mol Pharmacol. 2010 Jul;78(1):142-50.

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    Molecular Weight (MW)555.46
    FormulaC30H27BrN4O2
    CAS No.226929-39-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (180.0 mM)
    Water: <1 mg/mL
    Ethanol: 86 mg/mL warmed (154.8 mM)
    Other info

    Chemical Name: (1-((1-(4-bromobenzyl)-1H-imidazol-5-yl)methyl)-4-(naphthalen-1-yl)-1H-pyrrol-3-yl)(morpholino)methanone

    InChi Key: GUUIRIMAQGOLHT-UHFFFAOYSA-N

    InChi Code: InChI=1S/C30H27BrN4O2/c31-24-10-8-22(9-11-24)17-35-21-32-16-25(35)18-33-19-28(27-7-3-5-23-4-1-2-6-26(23)27)29(20-33)30(36)34-12-14-37-15-13-34/h1-11,16,19-21H,12-15,17-18H2

    SMILES Code: O=C(C1=CN(CC2=CN=CN2CC3=CC=C(Br)C=C3)C=C1C4=C5C=CC=CC5=CC=C4)N6CCOCC6           

    SynonymsLB-42708; LB 42708; LB42708; 


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    In Vitro

    In vitro activity: LB42708 potently inhibits the processing of the cellular farnesylated protein p21ras induced by LPS + IFN-γ in murine macrophage cell line RAW264.7 cells. LB42708 inhibits NF-κB activation and iNOS promoter activity through the inhibition of IKK activity. Moreover, LB42708 suppresses the expression of inducible NO synthase, cyclooxygenase-2, TNF-alpha, and IL-1beta and the production of NO and PGE(2) in immune-activated macrophages and osteoblasts. LB42708 irreversibly inhibits growth and induces apoptosis in H-ras and K-ras-transformed rat intestinal epithelial cells. LB42708 inhibits of VEGF-induced tumor angiogenesis by blocking Ras-dependent MAPK and PI3K/Akt pathways in tumor-associated endothelial cells.


    Cell Assay: Cell growth is measured by MTT. Briefly, cells were seeded at 2 × 103 cells per well in 96-well culture plates in triplicate. After the addition of various concentrations of drugs, cells are incubated for 72 h. At the end of culture, the plates are washed twice with PBS, and cells are incubated with 200 μl of RPMI 1640 containing 10% FCS and 0.25 mg/ml of MTT at 37 °C for 3 h. The absorbance of each well is measured with Titer-Tech 96-well multiscanner at 570 nm. The viable cell number is proportional to the absorbance.

    In VivoLB42708 (12.5 mg/kg i.p.) inhibits production of NO, PGE2, TNF-α, and IL-1β in LPS-injected mice, and also prevents the development of CIA. LB42708 (20 mg/kg/day i.p.) also inhibits tumor growth and angiogenesis in both Ras wild-type and mutated tumors.
    Animal modelMice collagen-induced arthritis model.
    Formulation & DosageDissolved in Saline; 10 mg/kg; i.p. injection
    References

    J Immunol. 2004 Jul 15;173(2):1276-83; Toxicol Appl Pharmacol. 2006 Sep 15;215(3):317-29; Mol Pharmacol. 2010 Jul;78(1):142-50.


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

    LB42708

    LB42708 inhibits VEGF-induced in vitro angiogenesis. Mol Pharmacol. 2010 Jul;78(1):142-50. 
     

    LB42708

    LB42708 inhibits VEGF-induced angiogenesis ex vivo and in vitro. Mol Pharmacol. 2010 Jul;78(1):142-50. 
     

    LB42708

    LB42708 regulates the VEGF-induced angiogenic signaling pathway. Mol Pharmacol. 2010 Jul;78(1):142-50. 
     

    LB42708

    Specific knockdown of FTase and Ras inhibits VEGF-induced signal transduction and in vitro angiogenesis. Mol Pharmacol.2010 Jul;78(1):142-50. 
     

    LB42708

    LB42708 and Ras knockdown blocks VEGF-induced endothelial cell cycle progression by arresting cells at the G1 phase. Mol Pharmacol. 2010 Jul;78(1):142-50. 
     

    LB42708

    LB42708 reduces tumor growth and angiogenesis in human tumor xenograft models. Mol Pharmacol. 2010 Jul;78(1):142-50. 


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