Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
IC50: 21 nM (GGTase I)[1]
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ln Vitro |
GGTI-2154 has an IC50 of 21 nM and prevents the transfer of geranylgeranyl from [3H]GGPP to H-Ras CVLL[1].
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ln Vivo |
In MMTV-v-Ha-Ras transgenic mice, GGTI-2154 (100 mg/kg/day; sc for 14 days) causes regression of breast tumors[2]. In nude mice, GGTI-2154 (50 mg/kg/day; ip for 50 days) suppresses the formation of A-549 tumors by 60%[1].
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Animal Protocol |
Animal/Disease Models: MMTV-v-Ha-ras transgenic mice bearing mammary carcinoma[2]
Doses: 100 mg/kg/day Route of Administration: Sc with osmotic mini-pumps for 14 days Experimental Results: Halted the tumors aggressive growth. Resulted in rapid tumor regression within 3 days of initiation of drug treatment. |
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.
[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. |
Molecular Formula |
C24H29CLN4O3
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Molecular Weight |
456.97
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CAS # |
478908-50-8
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Related CAS # |
GGTI-2154;251577-10-3
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
Cl.OC([C@H](CC(C)C)NC(C1C=CC(=CC=1C1C=CC=CC=1C)NCC1=CN=CN1)=O)=O
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : 250 mg/mL (547.08 mM)
H2O : 4.76 mg/mL (10.42 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 25 mg/mL (54.71 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 250.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 25 mg/mL (54.71 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 250.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 25 mg/mL (54.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1883 mL | 10.9416 mL | 21.8833 mL | |
5 mM | 0.4377 mL | 2.1883 mL | 4.3767 mL | |
10 mM | 0.2188 mL | 1.0942 mL | 2.1883 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.