| Description | FGTI-2734 is a dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor, exhibiting IC50 values of 250 nM and 520 nM for FT and GGT-1, respectively. It effectively prevents the membrane localization of KRAS, addressing the issue of KRAS resistance and inhibiting the growth of mutant KRAS patient-derived pancreatic tumors. |
| In vitro | FGTI-2734 (3-30 μM; 72小时) 抑制HDJ2、RAP1A、KRAS和NRAS的蛋白质前脂化。同时，FGTI-2734 在RAS转化的小鼠NIH3T3细胞和突变型KRAS人类癌细胞中抑制KRAS的膜定位。此外，FGTI-2734 (1-30 μM; 72小时) 在MiaPaCa2、L3.6pl和Calu6细胞中诱导CASPASE-3和PARP裂解。 |
| In vivo | FGTI-2734（腹腔注射；100 mg/kg/每日，持续18至25天）特异性抑制突变型KRAS依赖的肿瘤生长，对于非突变型KRAS依赖的肿瘤则无影响。 |
| Target activity | FTase:250 nM , GGTase I:520 nM |
| molecular weight | 510.63 |
| Molecular formula | C26H31FN6O2S |
| CAS | 1247018-19-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (97.92 mM), Sonication is recommended. |
| References | 1. Kazi A, et al. Dual farnesyl and geranylgeranyl transferase inhibitor thwarts mutant KRAS-driven patient-derived pancreatic tumors. Clin Cancer Res. 2019 Jun 21. |