Lonafarnib 193275-84-2

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Molecular Weight:

638.82 Lonafarnib is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Phase 3.






Biological 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


SCH66336 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.

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Product Categories : Metabolism > Transferase Inhibitor