Description
Lonafarnib is an inhibitor of farnesyl transferase (FT) with IC50 values of 1.9, 2.8, 5.2 and 10-100 nM for H-Ras, N-Ras, K-Ras and Rheb, respectively.
Product Overview
Lonafarnib (SCH66336, Sarasar) is an potent, selective, orally, bioavailable tricyclic nonpeptidyl nonsulfhydry inhibitor of farnesyltransferase (FTase). It is a small molecular with the formula of C27H31Br2ClN4O2 and molecular weight of 638.82.Farnesylated Ras proteins was found to regulate signal transduction pathways which drive cell proliferation, growth and survival and be required for its membrane localization. Lonafarnib inhibits the post-translational farnesylcation of ras proteins, therefore blocking translocation of RAS to the plasma membrane.
Synonyms
Sch 66336, Sch66336, Sch-66336
IC50
1.9 nM (H-Ras); 2.8 nM (N-Ras); 5.2 nM (K-Ras); 10-100 nM (Rheb)
Molecular Formula
C27H31Br2ClN4O2
Chemical Name
4-[2-[4-[(11R)-3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[1,2]cyclohepta[2,4-b]pyridin-11-yl]piperidin-1-yl]-2-oxoethyl]piperidine-1-carboxamide
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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