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Lonafarnib (SCH66336)
Catalog No.S2797
For research use only.
Lonafarnib (SCH66336) 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.
CAS No. 193275-84-2
Selleck's Lonafarnib (SCH66336) has been cited by 17 publications
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Biological Activity
| Description | Lonafarnib (SCH66336) 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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| Targets |
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| In vitro |
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. [2] SCH66336 demonstrate variable antiproliferative effects against the cell lines, with IC50 ranging from 0.6 μM to 32.3 μM. [3] 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.[4] |
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| Cell Data |
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| Assay |
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| In vivo | SCH66336 inhibits HTBI77 human lung carcinoma xenograft growth in nude mice in a dose-dependent fashion. [1] 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. [3] |
Protocol (from reference)
| Cell Research:[2] |
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Solubility (25°C)
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In vitro |
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Chemical Information
| Molecular Weight | 638.82 | ||
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| Formula | C27H31Br2ClN4O2 |
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| CAS No. | 193275-84-2 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | C1CN(CCC1CC(=O)N2CCC(CC2)C3C4=C(CCC5=C3N=CC(=C5)Br)C=C(C=C4Br)Cl)C(=O)N | ||
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT02579044 | Enrolling by invitation | Drug: Everolimus and lonafarnib | Progeria | Boston Children''s Hospital | December 2015 | Phase 1|Phase 2 |
| NCT02527707 | Completed | Drug: lonafarnib|Drug: Ritonavir | Chronic Delta Hepatitis | Eiger BioPharmaceuticals|Hannover Medical School | September 2015 | Phase 2 |
| NCT02430194 | Completed | Drug: lonafarnib|Drug: Ritonavir|Drug: PEG IFN-a | Chronic Hepatitis D Infection | Eiger BioPharmaceuticals|Ankara University | December 2014 | Phase 2 |
| NCT02430181 | Completed | Drug: lonafarnib|Drug: PEG IFN-a|Drug: Ritonavir | Chronic Hepatitis D Infection | Eiger BioPharmaceuticals | November 2014 | Phase 2 |
| NCT01495585 | Completed | Drug: Lonafarnib|Other: Placebo | Hepatitis D | National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Institutes of Health Clinical Center (CC) | December 2011 | Phase 2 |
| NCT01232881 | Terminated | Procedure: Tumor Sample|Procedure: Serum Sample | Breast Cancer | Hoosier Cancer Research Network|United States Department of Defense|Indiana University School of Medicine|Emory University | August 2009 | -- |
(data from https://clinicaltrials.gov, updated on 2022-08-01)
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