FGTI-2734

FGTI-2734CAS号: 1247018-19-4分子式: C26H31FN6O2S分子量: 510.63描述储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors. FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT-1, respectively.
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO:50 mg/mL (97.92 mM)
生物活性
靶点
Farnesyl transferase (FTase):250 nM, GGTase I:520 nM
In vitro(体外研究)
FGTI-2734 (3-30 μM;?72 hours) inhibits both protein prenylation of HDJ2, RAP1A, KRAS and NRAS.?FGTI-2734 inhibits KRAS membrane localization in RAS-transformed murine NIH3T3 cells and in mutant KRAS human cancer cells.?FGTI-2734 (1-30 μM;?72 hours) induces CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells.
In vivo(体内研究)
FGTI-2734 (intraperitoneally;?100 mg/kg/daily for 18 to 25 days) only inhibits tumor growth in mutant KRAS-dependent tumors but not in mutant KRAS-independent tumors.