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.
Purity & Quality Control
Choose Selective Transferase Inhibitors
|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)|
|Water||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|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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