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Purity: ≥98%
Bazedoxifene acetate (formerly TSE-424; WAY140424; WAY-140424; TSE424; Viviant), the acetic acid salt form of Bazedoxifene, is a 3rd generation selective estrogen receptor modulator (SERM) with IC50s of 26 and 99 nM for ERα and ERβ, respectively. In 2013, Bazedoxifene gained FDA approval as part of the combination drug Duavee used for the prevention of postmenopausal osteoporosis.
| ln Vitro |
Bazedoxifene acetate is a small molecular GP130 inhibitor, which binds to GP130 D1 domain[1]. Bazedoxifene acetate suppresses STAT3 phosphorylation produced by Il-6 and IL-11 in GP130/STAT3 pathway signaling[1]. Bazedoxifene acetate (10 μM -20 μM; 2 hours) inhibits STAT3 Phosphorylation Induced by cytokines in human pancreatic cancer cells[2]. Bazedoxifene acetate (5-20 μM; overnight) causes apoptosis in human pancreatic cancer cells[2]. Bazedoxifene acetate inhibits STAT3 nuclear translocation caused by IL-6[2]. Bazedoxifene acetate blocks the cells migration in pancreatic cancer cells by inhibition of GP130[2].
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| ln Vivo |
In a mouse model, benzodiazepine acetate (5 mg/kg; ig; daily, for 18 days) inhibits the growth of Capan-1 tumors in vivo[2].
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| Cell Assay |
Western Blot Analysis[2]
Cell Types: AsPC-1 cells Tested Concentrations: 10 μM, 20 μM Incubation Duration: 2 hrs (hours) Experimental Results: Inhibited IL-6, IL-11 or OSM (50 ng/mL) induced STAT3 phosphorylation. Apoptosis Analysis[2] Cell Types: Capan-1 cells, BxPC-3 cells, HPAF-II cells, HPAC cells Tested Concentrations: 10 μM, 20 μM (Capan-1); 5 μM, 10 μM (BxPC-3); 10 μM, 20 μM (HPAF-II); 10 μM, 15 μM (HPAC) Incubation Duration: Overnight Experimental Results: Induced apoptosis. |
| Animal Protocol |
Animal/Disease Models: 6weeks old female athymic nude mice[2]
Doses: 5 mg /kg Route of Administration: po (oral gavage), daily, for 18 days Experimental Results: Suppressed pancreatic cancer xenograft tumor growth and induced apoptosis in tumor cells. |
| References |
[1]. Barry S Komm, et al. Bazedoxifene acetate: a selective estrogen receptor modulator with improved selectivity. Endocrinology. 2005 Sep;146(9):3999-4008.
[2]. Xiaojuan Wu, et al. Bazedoxifene as a Novel GP130 Inhibitor for Pancreatic Cancer Therapy. Mol Cancer Ther. 2016 Nov; 15(11): 2609–2619. |
| Molecular Formula |
C30H34N2O3.HCL
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| Molecular Weight |
507.06
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| CAS # |
198481-33-3
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| Related CAS # |
Bazedoxifene;198481-32-2;Bazedoxifene hydrochloride;198480-56-7
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| SMILES |
CC1=C(C2=CC=C(O)C=C2)N(CC3=CC=C(OCCN4CCCCCC4)C=C3)C5=CC=C(O)C=C51.CC(O)=O
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| InChi Key |
OMZAMQFQZMUNTP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C30H34N2O3.C2H4O2/c1-22-28-20-26(34)12-15-29(28)32(30(22)24-8-10-25(33)11-9-24)21-23-6-13-27(14-7-23)35-19-18-31-16-4-2-3-5-17-31;1-2(3)4/h6-15,20,33-34H,2-5,16-19,21H2,1H3;1H3,(H,3,4)
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| Chemical Name |
1-(p-(2-(Hexahydro-1H-azepin-1-yl)ethoxy)benzyl)-2-(p-hydroxyphenyl)-3-methylindol-5-ol acetic acid
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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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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9722 mL | 9.8608 mL | 19.7215 mL | |
| 5 mM | 0.3944 mL | 1.9722 mL | 3.9443 mL | |
| 10 mM | 0.1972 mL | 0.9861 mL | 1.9722 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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