CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity.The IC 50 for inhibiting farnesylation of recombinant human H-Ras is 0.57 ng/mL and recombinant K-Ras is 46 ng/mL. In Vitro CP-609754 (CP-609,754) is a reversible inhibitor of farnesyltransferase with a slow on/off rate. CP-609,754 inhibits farnesylation (IC 50 =1.72 ng/mL) of mutant H-Ras in 3T3 H-ras (61L)-transfected cell lines with SDS-PAGE analysis of [ 35 S]methionine-labeled material. CP-609754 is competitive for the prenyl acceptor (H-Ras protein) and noncompetitive for the prenyl donor farnesyl PPI. CP-609754 interacts with the farnesyltransferase-farnesyl PPI complex and competes for the binding of the Ras protein. CP-609754 selectively inhibits farnesylation of both H- and K-Ras proteins in 3T3 transfectants. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo CP-609754 (CP-609,754) has antitumor activity against 3T3 H-ras (61L) tumors in vivo . With twice daily oral dosing of CP-609754, tumor regression is achieved with a dose of 100 mg/kg; the ED 50 for tumor growth inhibition is 28 mg/kg . With continuous i.p. infusion of CP-609754, tumor growth is inhibited by >50%, and tumor farnesyltransferase activity inhibited by >30% in mice in which the plasma concentration of CP-609754 is maintained above 118 ng/mL . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
CP-609754
CAS number：1190094-64-4 molecular formula：C29H22ClN3O2
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | CP-609754(OSI754) | OSI-754 | (R)-6-((4-chlorophenyl)(hydroxy)(1-methyl-1H-imidazol-5-yl)methyl)-4-(3-ethynylphenyl)-1-methylquinolin-2(1H)-one | EX-A4802 | AKOS040756201 | 2(1H)-QUINOLINONE, 6-((R)-(4-CHLOROPHENYL)HYDROXY(1-METHYL-1H-IMIDAZOL-5-YL)METHYL | ||
| CAS number | 1190094-64-4 | molecular formula | C29H22ClN3O2 |
| molecular weight | 479.96 g/mol | Exact mass | ≥99% |
| PSA | 58.400 Ų | logp | 4.000 |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
No safety information yet
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
