Catalog No.S2797 Synonyms: SCH66336
Molecular Weight(MW): 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 in cell-free assays, respectively. Phase 3.
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|Description||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 in cell-free assays, respectively. Phase 3.|
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.
|In vivo||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. |
|In vitro||DMSO||127 mg/mL (198.8 mM)|
|Ethanol||127 mg/mL (198.8 mM)|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02511431||Recruiting||Hepatitis D||National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Institutes of Health Clinical Center (CC)||July 21, 2015||Phase 2|
|NCT02968641||Not yet recruiting||Chronic Delta Hepatitis||Eiger BioPharmaceuticals||March 2017||Phase 2|
|NCT02579044||Recruiting||Progeria||Boston Children’s Hospital||December 2015||Phase 1|Phase 2|
|NCT02527707||Completed||Chronic Delta Hepatitis||Eiger BioPharmaceuticals|Hannover Medical School||September 2015||Phase 2|
|NCT02430194||Recruiting||Chronic Hepatitis D Infection||Eiger BioPharmaceuticals|Ankara University||December 2014||Phase 2|
|NCT02430181||Completed||Chronic Hepatitis D Infection||Eiger BioPharmaceuticals||November 2014||Phase 2|
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