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GGTI-2418 is a highly potent, competitive, and selective inhibitor of geranylgeranyltransferase I (GGTase I), exhibiting inhibitory activities with IC50 values of 9.5 nM for GGTase I and 53 μM for FTase, respectively. Additionally, it enhances p27(Kip1) expression and induces significant regression of breast tumors.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $48 | - | In Stock | |
| 5 mg | $113 | - | In Stock | |
| 10 mg | $189 | - | In Stock | |
| 25 mg | $372 | - | In Stock | |
| 50 mg | $562 | - | In Stock | |
| 100 mg | $790 | 7-10 days | 7-10 days | |
| 500 mg | $1,670 | 7-10 days | 7-10 days |
| Description | GGTI-2418 is a highly potent, competitive, and selective inhibitor of geranylgeranyltransferase I (GGTase I), exhibiting inhibitory activities with IC50 values of 9.5 nM for GGTase I and 53 μM for FTase, respectively. Additionally, it enhances p27(Kip1) expression and induces significant regression of breast tumors. |
| Targets&IC50 | GGTase I:9.5 nM, FTase:53 μM |
| In vitro | In HeLa cells, GGTI-2418 (10-15 μM; 16 hours) can delocalize FBXL2 and stabilize IP3R3[2]. |
| In vivo | GGTI-2418 (100 mg/kg daily; 5 days) induces regression of ErbB2-driven mammary tumors in ErbB2 transgenic mice. GGTI-2418 inhibits the geranylgeranylation of Rap1, significantly reduces Akt S473 phosphorylation, and upregulates p27 levels in vivo. Additionally, GGTI-2418 (100 mg/kg daily or 200 mg/kg every third day; 15 days) significantly inhibits the growth of MDA-MB-231 breast tumor xenografts in nude mice. |
| Synonyms | GGTI2418, GGT 2418 |
| Molecular Weight | 441.52 |
| Formula | C23H31N5O4 |
| Cas No. | 501010-06-6 |
| Smiles | CC(C)C[C@H](NC(=O)N1CCN(Cc2nc[nH]c2C)C(=O)[C@@H]1Cc1ccccc1)C(O)=O |
| Relative Density. | 1.270 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (226.49 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (9.06 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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