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LB42708

CAS No. 226929-39-1

LB42708( LB42708 | LB-42708 | LB 42708 )

Catalog No. M17445 CAS No. 226929-39-1

LB42708 is an orally active farnesyltransferase (FTase) inhibitor (IC50: 0.8/1.2/2.0 nM toward H/N/K-ras).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    LB42708
  • Note
    Research use only, not for human use.
  • Brief Description
    LB42708 is an orally active farnesyltransferase (FTase) inhibitor (IC50: 0.8/1.2/2.0 nM toward H/N/K-ras).
  • Description
    LB42708 is a potent, orally active and selective nonpeptidic farnesyltransferase inhibitor (FTase inhibitor). LB42708 inhibited VEGF-induced Ras activation and subsequently suppressed angiogenesis in vitro and in vivo by blocking the mitogen-activated protein kinase kinase/extracellular signal-regulated kinase/p38 mitogen-activated protein kinase (MAPK) and phosphatidylinositol 3-kinase (PI3K)/Akt/endothelial nitric-oxide synthase pathways in endothelial cells without altering FAK/Src activation.
  • In Vitro
    LB42708 induces cell death despite K-ras prenylation. Growth inhibition by LB42708 is accompanied by G1 and G2/M cell cycle arrests in H-ras and K-ras-transformed RIE cells, respectively. LB42708 induces the upregulation of p21(CIP1/WAF1) and RhoB above the basal level that leads to the cell cycle arrest and to distinct morphological alterations of ras-transformed rat intestinal epithelial (RIE) cells.
  • In Vivo
    ——
  • Synonyms
    LB42708 | LB-42708 | LB 42708
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Farnesyl transferase (FTase)| Farnesyl transferase (FTase)| Farnesyl transferase (FTase)
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    226929-39-1
  • Formula Weight
    555.46
  • Molecular Formula
    C30H27BrN4O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (180.03 mM)
  • SMILES
    Brc1ccc(Cn2cncc2Cn2cc(C(=O)N3CCOCC3)c(c2)c2cccc3ccccc23)cc1
  • Chemical Name
    (1-((1-(4-bromobenzyl)-1H-imidazol-5-yl)methyl)-4-(naphthalen-1-yl)-1H-pyrrol-3-yl)(morpholino)methanone

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Na HJ, et al. J Immunol. 2004, 173(2), 1276-1283.
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