FGTI-2734 |
| رقم الكتالوجGC36038 |
FGTI-2734 عبارة عن مثبط ثنائي فارنيسيل ترانسيلاز (FT) لمحاكاة RAS C ومحاكاة geranylgeranyl transferase-1 (GGT-1) مع IC50s من 250 نانومتر و 520 نانومتر لـ FT و GGT-1 ، على التوالييمكن لـ FGTI-2734 منع توطين غشاء KRAS ، وبالتالي حل مشكلة مقاومة KRAS وإحباط أورام البنكرياس المتحولة المشتقة من المريض KRAS
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1247018-19-4
Sample solution is provided at 25 µL, 10mM.
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FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT, respectively. FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors[1]. IC50: 250 nM (FT) and 520 nM (GGT)[1]
FGTI-2734 (1-30 μM; 72 hours) induces CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells[1]. 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[1]. Apoptosis Analysis[1] Cell Line: MiaPaCa2, L3.6pl and Calu6 cells
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[1]. Animal Model: Male SCID-bg mice following injection of MiaPaCa2, L3.6pl, Calu6, A549, H460 and DLD1 cancer cells[1]
[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.
| Cas No. | 1247018-19-4 | SDF | |
| Canonical SMILES | O=S(C1=NC=CC=C1)(N(CCN(C2=CC=C(C#N)C=C2F)CC3=CN=CN3C)CC4CCCCC4)=O | ||
| Formula | C26H31FN6O2S | M.Wt | 510.63 |
| الذوبان | DMSO: 50 mg/mL (97.92 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9584 mL | 9.7918 mL | 19.5837 mL |
| 5 mM | 391.7 μL | 1.9584 mL | 3.9167 mL |
| 10 mM | 195.8 μL | 979.2 μL | 1.9584 mL |
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- Purity: >99.00%
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