| Chemical Name |
FTI-2148 |
| CAS Number |
251577-09-0 |
| MDL Number |
MFCD08056245 |
| Molecular Formula |
C24H28N4O3S |
| Molecular Weight |
452.57 |
Introduction of 251577-09-0 :
FTI-2148 is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively[1]. IC50 & Target: IC50: 1.4 nM (FT-1); 1.7 μM (GGT-1)[1] In Vitro: FTI-2148 (30 μM) inhibits the farnesylation of the exclusively farnesylated protein HDJ2 in all 3 RAS-transformed NIH3T3 cells[1].
FTI-2148 is against P. falciparum PFT, Mammalian PFT and Mammalian PGGT-I with IC50 values of 15 nM; 0.82 nM and 1700 nM, respectively. PFT:protein farnesyltransferase; PGGT-I geranylgeranyltransferase-I[2].
In Vivo: FTI-2148 (intraperitoneal injection; 25 or 50 mpk/day with a mini-pump; started on day 15 and stopped on day 45 and restarted day 53-83) inhibits the tumor growth by 91% in human lung adenocarcinoma A-549 cells induced mouse model[1].
FTI-2148 (subcutaneous injection; 25 mpk/day with a mini-pump; 14 days) inhibits tumor growth by 77%by the end of the 2-week treatment in Human Xenograft Nude Mouse Model[1].
FTI-2148 (subcutaneous injection; 100 mg/kg/day; 14 days) results in breast tumor regression in a ras transgenic mouse model[1].
FTI-2148 (subcutaneous injection; 100 mg/kg/day; 4 days) results in 85–88% inhibition of FTase with no inhibition of GGTase I enzymatic activity in breast tumors from mice in vivo settings[3].
| Purity |
NLT 98% |
| Storage |
at 20ºC 2 years |
*The above information is for reference only.
