GGTI-2418 demonstrates competitive inhibition of GGTase I against the H-Ras-CVLL protein with a Ki of 4.4±1.6 nM.?GGTi-2418 (10-15 μM;?16 hours) treatment delocalizes FBXL2 and stabilizes IP3R3.GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5±2.0 nM and 53±11 μM, respectively, a 5,600-fold selectivity toward inhibition of GGTase I versus FTase.

GGTI-2418 (100 mg/kg daily; 5 days) induces regression of ErbB2-driven mammary tumors in ErbB2 transgenic mice. ?GGTI-2418 inhibits the geranylgeranylation of Rap1 and causes a dramatic decrease in S473 phosphorylation of Akt. GGTI-2418 also upregulates p27 levels in vivo.GGTI-2418 (100 mg/kg daily or 200 mg/kg every third day;?15 days) significantly inhibits the growth of breast tumor xenografts in nude mice with MDA-MB-231 xenografts.

501010-06-6

C23H31N5O4

441.52

DMSO:125 mg/mL (283.11 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years