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| 25mg |
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Purity: ≥98%
S-Gboxin is an analogue of Gboxin with anticancer activity by potently inhibiting growth of mouse and human glioblastoma (GBM) (IC50 = 470 nM). S-Gboxin is a novel and potent small molecule that specifically inhibits the growth of primary mouse and human glioblastoma cells but not that of mouse embryonic fibroblasts or neonatal astrocytes. Gboxin rapidly and irreversibly compromises oxygen consumption in glioblastoma cells. Gboxin relies on its positive charge to associate with mitochondrial oxidative phosphorylation complexes in a manner that is dependent on the proton gradient of the inner mitochondrial membrane, and it inhibits the activity of F0F1 ATP synthase. Gboxin-resistant cells require a functional mitochondrial permeability transition pore that regulates pH and thus impedes the accumulation of Gboxin in the mitochondrial matrix. Administration of a metabolically stable Gboxin analogue inhibits glioblastoma allografts and patient-derived xenografts. Gboxin toxicity extends to established human cancer cell lines of diverse organ origin, and shows that the increased proton gradient and pH in cancer cell mitochondria is a mode of action that can be targeted in the development of antitumour reagents.
| ln Vivo |
Excellent metabolic stability, improved plasma stability, and PK characteristics appropriate for in vivo research are all retained by S-Gboxin. Intraperitoneally administered S-Gboxin (10 mg/kg/day) suppresses the growth of glioblastoma (GBM) in vivo [1].
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| Animal Protocol |
Animal/Disease Models: Female nude mice (6 to 9 weeks) [1]
Doses: 10 mg/kg/day Route of Administration: intraperitoneal (ip) injection; daily; 3 or 14 days Experimental Results: Caused Dramatically attenuated growth and Cell density decreases. |
| References |
[1]. Shi Y, et al. Gboxin is an oxidative phosphorylation inhibitor that targets glioblastoma. Nature. 2019 Mar;567(7748):341-346.
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| Molecular Formula |
C27H32F3IN2O2
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|---|---|
| Molecular Weight |
600.454870223999
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| CAS # |
2101317-21-7
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| Related CAS # |
2101317-20-6 (cation);2101317-21-7 (iodide);
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| SMILES |
FC(C1=CC(C2=[N+](CC(O[C@H]3[C@H](C(C)C)CC[C@@H](C)C3)=O)C4=CC=CC=C4N2C)=CC=C1)(F)F.[I-]
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| InChi Key |
DCAJNAWCJSUZDG-DZJKTSMVSA-M
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| InChi Code |
InChI=1S/C27H32F3N2O2.HI/c1-17(2)21-13-12-18(3)14-24(21)34-25(33)16-32-23-11-6-5-10-22(23)31(4)26(32)19-8-7-9-20(15-19)27(28,29)30;/h5-11,15,17-18,21,24H,12-14,16H2,1-4H3;1H/q+1;/p-1/t18-,21+,24-;/m1./s1
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| Chemical Name |
3-(2-(((1R,2S,5R)-2-isopropyl-5-methylcyclohexyl)oxy)-2-oxoethyl)-1-methyl-2-(3-(trifluoromethyl)phenyl)-1H-benzo[d]imidazol-3-ium iodide
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| Synonyms |
S-Gboxin; S Gboxin
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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 : ~93.33 mg/mL (~155.43 mM)
H2O : ~1 mg/mL (~1.67 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 9.33 mg/mL (15.54 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 93.3 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: ≥ 9.33 mg/mL (15.54 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 93.3 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: ≥ 9.33 mg/mL (15.54 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 | 1.6654 mL | 8.3271 mL | 16.6542 mL | |
| 5 mM | 0.3331 mL | 1.6654 mL | 3.3308 mL | |
| 10 mM | 0.1665 mL | 0.8327 mL | 1.6654 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.
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