Effective Farnesyltransferase inhibitor (IC50 = 1.9 nM). Inhibition of Ras by Farnesitization. When used with CYTOTOXIC PGP substrate, PGP transport was also inhibited (IC50 & Lt; 3 μm) and its potency and anti-cancer activity were increased. Inhibit the
1.Taveras AG, Kirschmeier P, Baum CM. (2003) Sch-66336 (sarasar) and other benzocycloheptapyridyl farnesyl protein transferase inhibitors: discovery, biology and clinical observations.. Curr Top Med Chem, 3 (10):(1103-14). [PMID:12769711]
2.Gordon LB, Kleinman ME, Miller DT, Neuberg DS, Giobbie-Hurder A, Gerhard-Herman M, Smoot LB, Gordon CM, Cleveland R, Snyder BD et al.. (2012) Clinical trial of a farnesyltransferase inhibitor in children with Hutchinson-Gilford progeria syndrome.. Proc Natl Acad Sci USA, 109 (41):(16666-71). [PMID:23012407]
3.Young SG, Yang SH, Davies BS, Jung HJ, Fong LG. (2013) Targeting protein prenylation in progeria.. Sci Transl Med, 5 (171):(171ps3). [PMID:23390246]
4.Moorthy NS, Sousa SF, Ramos MJ, Fernandes PA. (2013) Farnesyltransferase inhibitors: a comprehensive review based on quantitative structural analysis.. Curr Med Chem, 20 (38):(4888-923). [PMID:24059235]
5.Gordon LB, Shappell H, Massaro J, D'Agostino Sr RB, Brazier J, Campbell SE, Kleinman ME, Kieran MW. (2018) Association of Lonafarnib Treatment vs No Treatment With Mortality Rate in Patients With Hutchinson-Gilford Progeria Syndrome.. JAMA, 319 (16):(1687-1695). [PMID:29710166]
6.Downward J. (2003) Targeting RAS signalling pathways in cancer therapy.. Nat Rev Cancer, 3 (1):(11-22). [PMID:12509763]
Solution Calculators
Molarity Calculator
Determine the necessary mass, volume, or concentration for preparing a solution.
Dilution Calculator
Determine the dilution needed to prepare a stock solution.
B2209334