FGTI-2734
Based on 1 publication(s) in Google Scholar
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. FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors.
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- Purity: 99.85%
- CAS No.: 1247018-19-4
- 화학식: C26H31FN6O2S
- 분자량:510.63
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보관:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Metabolism/Protease Compound Library
HY-L012
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Anti-Cancer Compound Library
HY-L025
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Anti-Pancreatic Cancer Compound Library
HY-L077
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Heterocyclic Compound Library
HY-L138
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Metabolic Enzyme Compound Library
HY-L146
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Anti-Drug-Resistant Compound Library
HY-L169
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Bioactive Compound Library Max
HY-L181
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HY-L001V
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HY-L001
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HY-L205
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Posttranslational Modification Library
HY-L226
Publications Citing Use of MedChemExpress (MCE) FGTI-2734
More
Biological Activity
IC50: 250 nM (FT) and 520 nM (GGT-1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NIH3T3 | IC50 |
0.0887 μM
Compound: 21b, FTI-2734
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Inhibition of H-Ras farnesylation expressed in mouse NIH3T3 cells
Inhibition of H-Ras farnesylation expressed in mouse NIH3T3 cells
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[PMID: 20822181] |
| NIH3T3 | IC50 |
2.7 μM
Compound: 21b, FTI-2734
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Inhibition of Rap1A geranylgeranylation expressed in mouse NIH3T3 cells
Inhibition of Rap1A geranylgeranylation expressed in mouse NIH3T3 cells
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[PMID: 20822181] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MiaPaCa2, L3.6pl and Calu6 cells
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Concentration:1, 3, 10, 30 μM
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Incubation Time:72 hours
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Result:Induced CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells.
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Cell Line:KRAS, HRAS, and NRAS-transformed NIH3T3 cells
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Concentration:3, 10, 30 μM
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Incubation Time:72 hours
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Result:Inhibited both protein prenylation of HDJ2, RAP1A, KRAS and NRAS.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male SCID-bg mice following injection of MiaPaCa2, L3.6pl, Calu6, A549, H460 and DLD1 cancer cells[1]
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Dosage:100 mg/kg
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Administration:Intraperitoneally; daily; for 18 to 25 days
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Result:Inhibited tumor growth in mutant KRAS-dependent tumors.
Chemical Information
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CAS No. 1247018-19-4
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Appearance Solid
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분자량 510.63
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화학식 C26H31FN6O2S
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Color White to off-white
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SMILES
O=S(C1=NC=CC=C1)(N(CCN(C2=CC=C(C#N)C=C2F)CC3=CN=CN3C)CC4CCCCC4)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
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J Alzheimers Dis
Regulation of glial ApoE secretion by the mevalonate pathway is independent of ApoE isoform. [Abstract]2025 Mar;104(2):473-487. PMID: 39994996
용액&용해도
DMSO : 50 mg/mL (97.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9584 mL | 9.7918 mL | 19.5837 mL | 48.9591 mL |
| 5 mM | 0.3917 mL | 1.9584 mL | 3.9167 mL | 9.7918 mL | |
| 10 mM | 0.1958 mL | 0.9792 mL | 1.9584 mL | 4.8959 mL | |
| 15 mM | 0.1306 mL | 0.6528 mL | 1.3056 mL | 3.2639 mL | |
| 20 mM | 0.0979 mL | 0.4896 mL | 0.9792 mL | 2.4480 mL | |
| 25 mM | 0.0783 mL | 0.3917 mL | 0.7833 mL | 1.9584 mL | |
| 30 mM | 0.0653 mL | 0.3264 mL | 0.6528 mL | 1.6320 mL | |
| 40 mM | 0.0490 mL | 0.2448 mL | 0.4896 mL | 1.2240 mL | |
| 50 mM | 0.0392 mL | 0.1958 mL | 0.3917 mL | 0.9792 mL | |
| 60 mM | 0.0326 mL | 0.1632 mL | 0.3264 mL | 0.8160 mL | |
| 80 mM | 0.0245 mL | 0.1224 mL | 0.2448 mL | 0.6120 mL |
FGTI-2734 Related Classifications
HY-128350 Related Classifications
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