GGTI-2154 hydrochloride
Based on 1 Customer Validation
GGTI-2154 hydrochloride is a potent and selective inhibitor geranylgeranyltransferase I (GGTase I), with an IC50 of 21 nM. GGTI-2154 hydrochloride shows more than 200-fold selectivity for GGTase I over FTase (IC50=5600 nM). GGTI-2154 hydrochloride can be used for the research of cancer.
For research use only. We do not sell to patients.
- Purity: 98.08%
- CAS No.: 478908-50-8
- Formula: C24H29ClN4O3
- Molecular Weight:456.97
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Bioactive Compound Library Max
HY-L181
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Bioactive Compound Library
HY-L001
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Apoptosis Compound Library
HY-L003
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Metabolism/Protease Compound Library
HY-L012
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Anti-Cancer Compound Library
HY-L025
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Mitochondrial Protection Compound Library
HY-L144
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Highly Selective Inhibitors Library
HY-L158
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Cell Death Library
HY-L162
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MCE Bioactive Compound Library
HY-L001V
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
IC50: 21 nM (GGTase I)[1]
GGTI-2154 (50 mg/kg/day; i.p. for 50 day) inhibits A-549 tumor growth in nude mice by 60%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MMTV-v-Ha-ras transgenic mice bearing mammary carcinoma[2]
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Dosage:100 mg/kg/day
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Administration:S.c. with osmotic mini-pumps for 14 days
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Result:Halted the tumors aggressive growth.
Resulted in rapid tumor regression within 3 days of initiation of drug treatment.
Chemical Information
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CAS No. 478908-50-8
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Appearance Solid
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Molecular Weight 456.97
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Formula C24H29ClN4O3
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Color White to off-white
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SMILES
CC(C)C[C@@H](C(O)=O)NC(C1=CC=C(NCC2=CN=CN2)C=C1C3=CC=CC=C3C)=O.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 250 mg/mL (547.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 4.76 mg/mL (10.42 mM; ultrasonic and warming and heat to 60°C)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 25 mg/mL (54.71 mM); Clear solution
This protocol yields a clear solution of ≥ 25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (250.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 25 mg/mL (54.71 mM); Clear solution
This protocol yields a clear solution of ≥ 25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (250.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 (sealed storage, away from moisture)
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.
Purity & Documentation
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Data Sheet (275 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
[1]. Sun J, et, al. Antitumor efficacy of a novel class of non-thiol-containing peptidomimetic inhibitors of farnesyltransferase and geranylgeranyltransferase I: combination therapy with the cytotoxic agents cisplatin, Taxol, and gemcitabine. Cancer Res. 1999 Oct 1;59(19):4919-26. [Content Brief]
[2]. Sun J, et, al. Geranylgeranyltransferase I inhibitor GGTI-2154 induces breast carcinoma apoptosis and tumor regression in H-Ras transgenic mice. Cancer Res. 2003 Dec 15;63(24):8922-9. [Content Brief]
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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.1883 mL | 10.9416 mL | 21.8833 mL | 54.7082 mL |
| 5 mM | 0.4377 mL | 2.1883 mL | 4.3767 mL | 10.9416 mL | |
| 10 mM | 0.2188 mL | 1.0942 mL | 2.1883 mL | 5.4708 mL | |
| DMSO | 15 mM | 0.1459 mL | 0.7294 mL | 1.4589 mL | 3.6472 mL |
| 20 mM | 0.1094 mL | 0.5471 mL | 1.0942 mL | 2.7354 mL | |
| 25 mM | 0.0875 mL | 0.4377 mL | 0.8753 mL | 2.1883 mL | |
| 30 mM | 0.0729 mL | 0.3647 mL | 0.7294 mL | 1.8236 mL | |
| 40 mM | 0.0547 mL | 0.2735 mL | 0.5471 mL | 1.3677 mL | |
| 50 mM | 0.0438 mL | 0.2188 mL | 0.4377 mL | 1.0942 mL | |
| 60 mM | 0.0365 mL | 0.1824 mL | 0.3647 mL | 0.9118 mL | |
| 80 mM | 0.0274 mL | 0.1368 mL | 0.2735 mL | 0.6839 mL | |
| 100 mM | 0.0219 mL | 0.1094 mL | 0.2188 mL | 0.5471 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
GGTI-2154 hydrochloride Related Classifications
HY-16229A Related Classifications
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