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GGTI-2418
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Catalog No. T11396Cas No. 501010-06-6
Alias GGTI2418, GGT 2418
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.
GGTI-2418
😃Good
Catalog No. T11396Alias GGTI2418, GGT 2418Cas No. 501010-06-6
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 | Availability | 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 | |
| 500 mg | $1,670 | 7-10 days |
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Product Introduction
Bioactivity
Chemical Properties
| 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. |
| Alias | 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 & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (226.49 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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