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Purity: ≥98%
Pantoprazole (BY1023; SKF96022; BY-1023; SKF-96022; Protonix), an approved anti-ulcer drug, is a proton pump inhibitor (PPI) used for short-term treatment of erosion and ulceration of the esophagus caused by GERD (gastroesophageal reflux disease). Pantoprazole acts by inhibiting the activity of H+/K+-ATPase proton pumb in the parietal cells of gastric mucosa. This inhibition affects the acid secretion and thus, pantoprazole are used as drugs for the treatment of various acid-related disorders. Pantoprazole is activated slowly. The activated sulfonamide of pantoprazole binds to Cys813 and Cys822 of the pumb and inhibits acid secretion selectively.
| ln Vitro |
In EMT-6 and MCF7 cells, pantoprazole (BY1023; 1–10,000 μM) causes concentration-dependent increases in endosomal pH[1]. BY10232, Pantoprazole, can prevent the release of exosomes. Pantoprazole (BY10232) reduces the ability of tumor cells (melanomas, adenocarcinomas, and lymphoma cell lines) to acidify the extracellular medium by blocking V-H+-ATPase activity[2].
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| ln Vivo |
When coupled with doxorubicin, pantoprazole (BY1023; 200 mg/kg; IP; once a week for three weeks) dramatically prolongs the tumor development delay of MCF-7 xenografts[1]. In rats with pylorus ligation, pantoprazole (0.3–3 mg/kg, po) dose-dependently reduces basal acid secretion, while in rats with acute fistula, mepirizole-stimulated acid secretion is reduced[4].
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| Animal Protocol |
Animal/Disease Models: Mice bearing MCF-7 or A431 xenografts[1]
Doses: 200 mg/kg Route of Administration: IP; once a week for 3 weeks; alone or 2 hrs (hours) before Doxorubicin (6 mg/kg iv) Experimental Results: demonstrated even greater growth delay of MCF-7 xenografts with Doxorubicin compared with the single-dose combination. Dramatically increased tumor growth delay with a single dose with Doxorubicin. There is no effect on growth delay alone. |
| References |
[1]. Krupa J Patel, et al. Use of the proton pump inhibitor pantoprazole to modify the distribution and activity of doxorubicin: a potential strategy to improve the therapy of solid tumors. Clin Cancer Res. 2013 Dec 15;19(24):6766-76.
[2]. Huarui Zhang, et al. Advances in the discovery of exosome inhibitors in cancer. J Enzyme Inhib Med Chem. 2020 Dec;35(1):1322-1330. [3]. W Beil, et al. Pantoprazole: a novel H+/K(+)-ATPase inhibitor with an improved pH stability. Eur J Pharmacol. 1992 Aug 6;218(2-3):265-71. [4]. K Takeuchi, et al. Effects of pantoprazole, a novel H+/K+-ATPase inhibitor, on duodenal ulcerogenic and healing responses in rats: a comparative study with omeprazole and lansoprazole. J Gastroenterol Hepatol. 1999 Mar;14(3):251-7. |
| Molecular Formula |
C16H15F2N3O4S
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| Molecular Weight |
383.37
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| CAS # |
102625-70-7
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| Related CAS # |
Pantoprazole sodium;138786-67-1;Pantoprazole sodium hydrate;164579-32-2;S-Pantoprazole sodium trihydrate;1416988-58-3;Pantoprazole-d6;922727-65-9;Pantoprazole-d3;922727-37-5
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| SMILES |
O=S(C1=NC2=CC=C(OC(F)F)C=C2N1)CC3=NC=CC(OC)=C3OC
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| InChi Key |
IQPSEEYGBUAQFF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H15F2N3O4S/c1-23-13-5-6-19-12(14(13)24-2)8-26(22)16-20-10-4-3-9(25-15(17)18)7-11(10)21-16/h3-7,15H,8H2,1-2H3,(H,20,21)
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| Chemical Name |
1H-Benzimidazole, 5-(difluoromethoxy)-2-(((3,4-dimethoxy-2-pyridinyl)methyl)sulfinyl)-
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.52 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 25.0 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: ≥ 2.5 mg/mL (6.52 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 25.0 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: ≥ 2.5 mg/mL (6.52 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 | 2.6084 mL | 13.0422 mL | 26.0845 mL | |
| 5 mM | 0.5217 mL | 2.6084 mL | 5.2169 mL | |
| 10 mM | 0.2608 mL | 1.3042 mL | 2.6084 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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