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Lonafarnib 
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
(CAS 193275-84-2)
Description:

Farnesyl transferase 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. By arresting growth, farnesyl transferase inhibitors have great potential as antitumor agents. Lonafarnib is a farnesyl transferase inhibitor that blocks the post-translational lipid modification of oncogenic Ras isoforms HRas, NRas, and KRas (IC50s = 1.9, 2.8, and 5.2 nM, respectively) as well as Rheb (IC50 = 10-100 nM).It inhibits HRas 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 KRas 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. 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.

 

Product No. KT20016 
Product Name Lonafarnib 
Synonyms Sarasar; Sch 66336; Sch-66336; Sch66336
Formal Name 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
CAS Number 193275-84-2
Molecular Formula C27H31Br2ClN4O2
Formula Weight 638.8
Formulation A crystalline solid
Purity 98%min
Stability 1 year
Storage -20°C
Shipping USD45 for Europe and USA. No shipping charge once amount reach USD500.
Quality Control HNMR,CNMR,LCMS,HPLC,IR,etc.
Price & Availability In Stock. Price Negotiated.
 
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