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Lonafarnib is a FPTase inhibitor. It can inhibit H-ras (IC50 = 1.9 nM), K-ras-4B (IC50 = 5.2 nM) and N-ras (IC50 = 2.8 nM).
Synonyms: Sch66336; Sarasar
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Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
CAS No. : | 193275-84-2 |
Formula : | C27H31Br2ClN4O2 |
M.W : | 638.82 |
SMILES Code : | O=C(N1CCC(CC(N2CCC([C@@H]3C4=C(Br)C=C(Cl)C=C4CCC5=CC(Br)=CN=C53)CC2)=O)CC1)N |
Synonyms : |
Sch66336; Sarasar
|
MDL No. : | MFCD06795138 |
InChI Key : | DHMTURDWPRKSOA-RUZDIDTESA-N |
Pubchem ID : | 148195 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
Target |
|
In Vitro:
Concentration | Treated Time | Description | Reference |
normal human dermal fibroblasts (NDFs) | 5 μM | 16 days | To investigate the effect of FTI-277 on progerin accumulation, results showed that FTI-277 significantly reduced progerin accumulation. | PMC11113360 |
C2C12 myotubes | 2 μM | 24 hours | Lonafarnib significantly improved myotube area, fusion index, and myotube diameter, indicating its protective effect against dexamethasone-induced muscle atrophy. | PMC11696026 |
HEp-2 cells | 5 μM | 48 hours | To screen the ReFRAME library and confirm the antiviral activity of Lonafarnib | PMC10853176 |
293 T cells | 5 μM | 48 hours | To evaluate the inhibitory effect of Lonafarnib on RSV F protein-induced cell fusion | PMC10853176 |
MCF-7 | 5 and 10 μM | 48 hours | To observe the effects of lonafarnib on microtubule structure, results showed that lonafarnib treatment led to increased microtubule bundling | PMC1861827 |
A549 | 5-20 μM | 48 hours | To assess the effects of lonafarnib on tubulin polymerization, results showed that lonafarnib treatment led to increased tubulin polymerization | PMC1861827 |
HEp-2 cells | 57.7 ± 15.4 nM ( EC50) | 72 hours | Lonafarnib inhibited RSV A2 and B01 genotypes with EC50 values of 57.7 ± 15.4 nM and 75.5 ± 4.0 nM, respectively. | PMC11163014 |
Human bronchial epithelial cells (HBEC) | 599.9 ± 67.4 nM ( EC50) | 72 hours | Lonafarnib inhibited RSV A2 and B01 replication in HBEC with EC50 values of 599.9 ± 67.4 nM and 515.0 ± 44.2 nM, respectively. | PMC11163014 |
SH-SY5Y | 1 μM | 72 hours | Lonafarnib in combination with ALK TKIs decreased cell viability and showed synergistic effects at higher concentrations | PMC11039739 |
KELLY | 1 μM | 72 hours | Lonafarnib in combination with ALK TKIs showed synergistic effects in KELLY cells, but additive effects at higher concentrations | PMC11039739 |
In Vivo:
Administration | Dosage | Frequency | Description | Reference |
Mice | RSV infection model | Oral | 60 mg/kg | twice daily for 4 days | To evaluate the effect of Lonafarnib on RSV virus load in mice, results showed that Lonafarnib significantly reduced the virus load | PMC10853176 |
BALB/c mice | RSV infection model | Oral | 17 or 34 mg/kg | Twice daily for 4 consecutive days | Lonafarnib significantly reduced RSV replication in the BALB/c mouse model, with a 7.4-fold decrease in viral titer at 34 mg/kg dose, and alleviated lung inflammation. | PMC11163014 |
NSG mice | COG-N-426x PDX model | Oral | 40 mg/kg | Daily for 30 days | Combination of lonafarnib with ceritinib significantly delayed tumor growth and showed strong synergistic effects during treatment, but tumors rapidly regrew after cessation of therapy | PMC11039739 |
Sprague-Dawley rats | Dexamethasone-induced muscle atrophy model | Intraperitoneal injection | 1 μM and 5 μM | Once daily for 6 days | Lonafarnib significantly improved grip strength, muscle weight, and compound muscle action potential (CMAP) amplitudes in dexamethasone-induced muscle atrophy models, indicating its mitigation of muscle atrophy through enhanced mitochondrial function and anabolic pathways. | PMC11696026 |
Mice | LmnaG609G/G609G mouse model | Oral | 450 mg/kg | Daily, throughout the survival period | To evaluate the effect of Lonafarnib on LmnaG609G/G609G mice, it was found to extend survival, improve body weight, and reduce kyphosis | PMC11488313 |
Mice | Hutchinson-Gilford progeria syndrome model | Oral | 450 mg/kg | Daily, from post-weaning (P21) or P100 to P168 days | Lonafarnib improved cardiovascular function and survival, significantly reducing pulse wave velocity and improving left ventricular diastolic function. | PMC10023154 |
Clinical Trial:
NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
NCT00040534 | Neoplasms | Phase 1 | Terminated | - | - |
NCT00040547 | Neoplasms | Phase 1 | Completed | - | - |
NCT00003956 | Lymphoma Unsp... More >>ecified Adult Solid Tumor, Protocol Specific Less << | Phase 1 | Completed | - | United States, New York ... More >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 Less << |
NCT00038493 | Glioblastoma Multiforme | Phase 2 | Completed | - | United States, Texas ... More >> UTMD Anderson Cancer Center Houston, Texas, United States, 77030 Less << |
NCT00038584 | Carcinoma, Squamous Cell ... More >> Cancer of Head and Neck Less << | Phase 1 | Completed | - | United States, Texas ... More >> The University of Texas M. D. Anderson Cancer Center Houston, Texas, United States, 77030 Less << |
NCT00034684 | Leukemia Myel... More >>odysplastic Syndromes Leukemia, Myeloid, Chronic Blast Crisis Leukemia, Lymphocytic Less << | Phase 1 Phase 2 | Completed | - | - |
NCT00038597 | Myelogenous Leukemia, Chronic | Phase 2 | Completed | - | United States, Texas ... More >> MDAnderson Cancer Center Houston, Texas, United States, 77030 Less << |
NCT00073450 | Carcinoma, Squamous Cell ... More >> Head and Neck Neoplasms Less << | Phase 2 | Terminated | - | - |
NCT00612651 | Gliosarcoma G... More >>lioblastoma Anaplastic Astrocytoma Less << | Phase 1 | Completed | - | United States, North Carolina ... More >> Duke University Health System Durham, North Carolina, United States, 27710 Less << |
NCT00020774 | Liver Cancer | Phase 2 | Withdrawn | - | - |
NCT00006351 | Bladder Cancer ... More >> Transitional Cell Cancer of the Renal Pelvis and Ureter Urethral Cancer Less << | Phase 2 | Completed | - | Netherlands ... More >> University Medical Center Nijmegen Nijmegen, Netherlands, 6500 Less << |
NCT00068757 | Breast Cancer | Phase 1 | Completed | - | Belgium ... More >> Institut Jules Bordet Brussels, Belgium, 1000 France Institut Curie Hopital Paris, France, 75248 Netherlands Netherlands Cancer Institute - Antoni van Leeuwenhoek Hospital Amsterdam, Netherlands, 1066 CX Less << |
NCT03719313 | Hepatitis Delta Virus | Phase 3 | Not yet recruiting | November 1, 2021 | - |
NCT00005030 | Colorectal Cancer ... More >> Metastatic Cancer Less << | Phase 1 | Withdrawn(No enrollment.) | - | - |
NCT00083096 | Brain and Central Nervous Syst... More >>em Tumors Less << | Phase 1 | Unknown | - | France ... More >> Centre de Lutte Contre le Cancer Georges-Francois Leclerc Dijon, France, 21079 Centre Regional Rene Gauducheau Nantes-Saint Herblain, France, 44805 Switzerland Centre Hospitalier Universitaire Vaudois Lausanne, Switzerland, CH-1011 Less << |
NCT00050336 | Carcinoma, Non-small-cell Lung... More >> Metastases, Neoplasm Less << | Phase 3 | Terminated | - | - |
NCT00102635 | Head and Neck Cancer | Phase 1 | Terminated(Slow accrual.) | - | United States, Texas ... More >> UT MD Anderson Cancer Center Houston, Texas, United States, 77030 Less << |
NCT03600714 | Liver Disease ... More >> Hepatitis D Less << | Phase 2 | Recruiting | December 31, 2025 | United States, Maryland ... More >> National Institutes of Health Clinical Center Recruiting Bethesda, Maryland, United States, 20892 Contact: For more information at the NIH Clinical Center contact Office of Patient Recruitment (OPR) ?? 800-411-1222 ext TTY8664111010 ?? prpl@cc.nih.gov Less << |
NCT02511431 | Hepatitis D | Phase 2 | Completed | - | United States, Maryland ... More >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 Less << |
NCT00281515 | Epithelial Ovarian Cancer | PHASE2 | COMPLETED | 2025-12-11 | Charité - Universit?tsmedizin ... More >>Berlin, Campus Virchow-Klinikum, Klinik für Frauenheilkunde, Berlin, 13353, Germany|Klinikum Bremen Mitte, Frauenklinik, Bremen, 28177, Germany|Carl-Gustav-Carus der TU Dresden, Universit?ts-Frauenklinik, Dresden, 01307, Germany|Ev. Krankenhaus, Frauenklinik, Düsseldorf, 40217, Germany|Klinik für Frauenheilkunde der Univ. Erlangen, Erlangen, 91054, Germany|Universit?tsfrauenklinik, Essen, 45147, Germany|Klinikum der Johann Wolfgang Goethe Universit?t, Klinik für Frauenheilkunde u. Geburtshilfe, Frankfurt, 60590, Germany|Universit?tsklinikum Freiburg, Frauenklinik, Freiburg, 79106, Germany|Kreiskrankenhaus, Frauenklinik, Gifhorn, 38518, Germany|Klinik u. Poliklinik für Gyn?kologie und Geburtshilfe, Greifswald, 17487, Germany|Medizinische Hochschule, Hannover, 30625, Germany|St. Vincentius-Krankenh?user, Karlsruhe, 76137, Germany|Universit?tsklinikum Schleswig-Holstein, Campus Kiel, Klinik für Gyn?kologie und Geburtshilfe, Kiel, 24105, Germany|Klinik der Otto-von-Guericke Universit?t, Frauenklinik, Magdeburg, 39108, Germany|Johannes-Gutenberg-Universit?t, Universit?ts-Frauenklinik, Mainz, 55101, Germany|Klinikum der Philipps-Universit?t Marburg, Klinik für Gyn?kologie, Gyn?kologische Endokrinologie, Marburg, 35037, Germany|Klinikum Gro?hadern, Frauenklinik, München, 81377, Germany|Klinikum rechts der Isar der TU München, München, 81675, Germany|Elblandkliniken, Frauenklinik, Radebeul, 01445, Germany|Klinikum Südstadt, Rostock, 18059, Germany|Universit?ts-Frauenklinik, Tübingen, 72076, Germany|Universit?tsfrauenklinik, Ulm, 89075, Germany|Dr. Horst Schmidt Klinik, Gyn?kologie u. Gyn?kologische Onkologie, Wiesbaden, 65199, Germany Less << |
NCT02511431 | - | Completed | - | - | |
NCT00015899 | Brain and Central Nervous Syst... More >>em Tumors Less << | Phase 1 | Completed | - | United States, California ... More >> UCSF Comprehensive Cancer Center San Francisco, California, United States, 94143-0372 United States, District of Columbia Children's National Medical Center Washington, District of Columbia, United States, 20010-2970 United States, Massachusetts Dana-Farber/Harvard Cancer Center at Dana Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, North Carolina Duke Comprehensive Cancer Center Durham, North Carolina, United States, 27710 United States, Pennsylvania Children's Hospital of Philadelphia Philadelphia, Pennsylvania, United States, 19104-4318 Children's Hospital of Pittsburgh Pittsburgh, Pennsylvania, United States, 15213 United States, Tennessee St. Jude Children's Research Hospital Memphis, Tennessee, United States, 38105-2794 United States, Texas Texas Children's Cancer Center Houston, Texas, United States, 77030-2399 United States, Washington Children's Hospital and Regional Medical Center - Seattle Seattle, Washington, United States, 98105 Less << |
NCT00288444 | Lung Cancer S... More >>oft Tissue Sarcoma Colorectal Carcinoma Breast Cancer Prostate Cancer Less << | Phase 1 | Terminated | - | United States, Georgia ... More >> Emory University Winship Cancer Institute Atlanta, Georgia, United States, 30308 Less << |
NCT00102648 | Malignant Supratentorial Neopl... More >>asm Recurrent Glioblastoma Recurrent Gliosarcoma Less << | Phase 1 | Active, not recruiting | December 1, 2020 | United States, Texas ... More >> M D Anderson Cancer Center Houston, Texas, United States, 77030 Less << |
NCT01232881 | - | Terminated(funding terminated) | - | United States, Indiana ... More >> Indiana University Melvin and Bren Simon Cancer Center Indianapolis, Indiana, United States, 46202 Less << | |
NCT00916747 | Progeria | Phase 2 | Enrolling by invitation | July 2020 | United States, Massachusetts ... More >> Children's Hospital Boston Boston, Massachusetts, United States, 02115 Less << |
NCT02430181 | Chronic Hepatitis D Infection | Phase 2 | Completed | - | Turkey ... More >> Ankara University Medical School Ankara, Turkey Less << |
NCT00047502 | Chronic Myelogenous Leukemia | Phase 1 | Completed | - | United States, Texas ... More >> M.D. Anderson Cancer Center Houston, Texas, United States, 77030 Less << |
NCT01495585 | Hepatitis D | Phase 2 | Completed | - | United States, Maryland ... More >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 Less << |
NCT01495585 | - | Completed | - | - | |
NCT00081510 | Breast Cancer | Phase 2 | Completed | - | - |
NCT02968641 | Chronic Delta Hepatitis | Phase 2 | Unknown | - | - |
NCT02430194 | Chronic Hepatitis D Infection | Phase 2 | Completed | - | Turkey ... More >> Ankara University Medical School Ankara, Turkey Less << |
NCT00539968 | Prostate Cancer ... More >> Breast Cancer Ovarian Cancer Lung Cancer Gastric Cancer Less << | Phase 1 Phase 2 | Terminated | - | - |
NCT00425607 | Progeria|Hutchinson-Gilford Sy... More >>ndrome Less << | PHASE2 | COMPLETED | 2025-10-09 | Children's Hospital Boston, Bo... More >>ston, Massachusetts, 02115, United States Less << |
NCT00879034 | Progeria Hutc... More >>hinson-Gilford Syndrome Less << | Phase 2 | Completed | - | United States, Massachusetts ... More >> Children's Hospital Boston Boston, Massachusetts, United States, 02115 Less << |
NCT00109538 | Myelodysplastic Syndromes ... More >> Leukemia, Myelomonocytic, Chronic Myelodysplasia Myelomonocytic Less << | Phase 3 | Terminated | - | - |
NCT00773474 | Metastatic Breast Cancer | PHASE2 | TERMINATED | 2025-11-10 | Medical & Surgical Specialists... More >>, LLC, Galesburg, Illinois, 61401, United States|Cancer Care Center of Southern Indiana, Bloomington, Indiana, 47403, United States|Indiana University Melvin and Bren Simon Cancer Center, Indianapolis, Indiana, 46202, United States|Arnett Cancer Care, Lafayette, Indiana, 47904, United States|Horizon Oncology Center, Lafayette, Indiana, 47905, United States|Ireland Cancer Center - University Hospitals of Cleveland, Cleveland, Ohio, 44106, United States Less << |
NCT00425607 | Progeria|Hutchinson-Gilford Sy... More >>ndrome Less << | PHASE2 | COMPLETED | 2025-10-09 | Children's Hospital Boston, Bo... More >>ston, Massachusetts, 02115, United States Less << |
NCT00773474 | Metastatic Breast Cancer | PHASE2 | TERMINATED | 2025-11-10 | Medical & Surgical Specialists... More >>, LLC, Galesburg, Illinois, 61401, United States|Cancer Care Center of Southern Indiana, Bloomington, Indiana, 47403, United States|Indiana University Melvin and Bren Simon Cancer Center, Indianapolis, Indiana, 46202, United States|Arnett Cancer Care, Lafayette, Indiana, 47904, United States|Horizon Oncology Center, Lafayette, Indiana, 47905, United States|Ireland Cancer Center - University Hospitals of Cleveland, Cleveland, Ohio, 44106, United States Less << |
NCT00879034 | - | Completed | - | - | |
NCT02527707 | Chronic Delta Hepatitis | Phase 2 | Completed | - | - |
NCT02579044 | Progeria | Phase 1 Phase 2 | Recruiting | December 2021 | United States, Massachusetts ... More >> Boston Children's Hospital Recruiting Boston, Massachusetts, United States, 02115 Contact: Monica E Kleinman, MD ?? ?? monica.kleinman@childrens.harvard.edu Less << |
NCT03895528 | Progeria|HGPS | APPROVED_FOR_MARKETING | - | - |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.57mL 0.31mL 0.16mL |
7.83mL 1.57mL 0.78mL |
15.65mL 3.13mL 1.57mL |
|
Dissolving Methods |
in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day; The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound. Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:
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