FTI-277 (hydrochloride)

FTI-277 is an inhibitor of farnesyltransferase (FTase; IC₅₀ = 0.1 µM).¹ It is selective for FTase over geranylgeranyl transferase (GGTase; IC₅₀= >10 µM). FTI-277 (10 µM) inhibits IL-1β-induced production of nitric oxide (NO) in primary rat pulmonary artery smooth muscle cells.² It decreases the proliferation of A549 lung cancer cells when used at a concentration of 10 µM and induces cell cycle arrest at the G₂/M phase in the same cells at 20 µM.³ Intracisternal administration of FTI-277 increases the diameter of basilar arteries, improves appetite, and increases activity in a dog model of subarachnoid hemorrhage-induced vasospasm.⁴

WARNING This product is not for human or veterinary use.

1. Lerner, E.C., Qian, Y., Blaskovich, M.A., et al. Ras CAAX peptidomimetic FTI-277 selectively blocks oncogenic Ras signaling by inducing cytoplasmic accumulation of inactive Ras-Raf complexes. The Journal of Biological Chemisty 270(45), 26802-26806 (1995).

2. Finder, J.D., Litz, J.L., Blaskovich, M.A., et al. Inhibition of protein geranylgeranylation causes a superinduction of nitric-oxide synthase-2 by interleukin-1β in vascular smooth muscle cells. The Journal of Biological Chemisty 272, 13484-13488 (1997).

3. Miquel, K., Pradines, A., Sun, J., et al. GGTI-298 induces G₀-G₁ block and apoptosis whereas FTI-277 causes G₂-M enrichment in A549 cells. Cancer Res. 57(10), 1846-1850 (1997).

4. Yamaguchi, M., Zhou, C., Nanda, A., et al. Ras protein contributes to cerebral vasospasm in a canine double-hemorrhage model. Stroke 35(7), 1750-1755 (2004).