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Lonafarnib

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    Lonafarnib
  • Lonafarnib
Cat No: 11746
Biochemicals - Small Molecule Inhibitors
Cayman

Farnesyltransferase drives the post-translational farnesylation of a number of target proteins, including Ras, a component of the MAPK and Akt signaling pathways involved in cell proliferation, and Ras homolog enriched in brain (Rheb), which stimulates...

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Territorial Availability: Available through Bertin Technologies only in France
Synonyms:
  • 4-[2-[4-[(11R)-3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl]-1-piperidinyl]-2-oxoethyl]-1-piperidinecarboxamide
Correlated keywords:
  • Sch66336 Sch-66336 farnesyl transferase post-translational modifications farnesylation Ras MAPK Akt cells proliferation Rheb mTOR antitumors anticancers inhibitors posttranslational post translational lipids oncogenic isoforms H-Ras HRas N-Ras NRas K-Ras KRas cytotoxic agents cyclophosphamide 5-fluorouracil vincristine in vivo inhibits inhibitions protein lipidation
Product Overview:
Farnesyltransferase drives the post-translational farnesylation of a number of target proteins, including Ras, a component of the MAPK and Akt signaling pathways involved in cell proliferation, and Ras homolog enriched in brain (Rheb), which stimulates mTOR activity.{21707} By arresting growth, farnesyltransferase inhibitors have great potential as antitumor agents. Lonafarnib is a farnesyltransferase inhibitor that blocks the post-translational lipid modification of oncogenic Ras isoforms H-Ras, N-Ras, and K-Ras (IC50s = 1.9, 2.8, and 5.2 nM, respectively) as well as Rheb (IC50 = 10-100 nM).{21709,21708} It inhibits H-Ras signaling in whole cells (IC50 = 10 nM) and blocks the transformed growth properties of fibroblasts (IC50 = 75 nM) and human tumor cell lines (IC50 = 400 nM) expressing activated K-Ras proteins. In the nude mouse, lonafarnib demonstrates potent dose-dependent oral activity in an array of human tumor xenograft models including tumors originating from colon, lung, pancreas, prostate, and urinary bladder.{21709} Combination treatments with various cytotoxic agents (cyclophosphamide, 5-fluorouracil, and vincristine) or MAPK or Akt pathway inhibitors can enhance the in vivo efficacy of lonafarib.{21709,21706}
Size 1 mg
Shipping dry ice
CAS Number 193275-84-2
Molecular Formula C27H31Br2ClN4O2
SMILES BrC1=CN=C([C@H](C2CCN(C(CC3CCN(C(N)=O)CC3)=O)CC2)C(C(Br)=CC(Cl)=C4)=C4CC5)C5=C1
Molecular Weight 638,8
Formulation A crystalline solid
Purity ≥98%
Custom Code 2908.99
UNSPSC code 12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.

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