| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Bazedoxifene HCl (formerly TSE-424; WAY-140424; WAY140424; TSE424; Viviant), the hydrochloride salt of Bazedoxifene, is a non-steroidal, indole-based and 3rd generation selective estrogen receptor modulator (SERM) with potential antineoplastic activity. It inhibits ERα and ERβ with IC50s of 23 nM and 89 nM, respectively. Bazedoxifene was approved by FDA in 2013 as part of the combination drug Duavee used for the prevention of postmenopausal osteoporosis.
| ln Vitro |
Small-molecule GP130 inhibitor benzedoxifene hydrochloride interacts to the GP130 D1 domain[1]. In the GP130/STAT3 pathway signaling, benzodiazepine hydrochloride suppresses the phosphorylation of STAT3 that is triggered by IL-6 and IL-11[1]. In human pancreatic cancer cells, benzodiazepine hydrochloride (10 μM–20 μM; 2 hours) suppresses the phosphorylation of STAT3 caused by cytokines[2]. Bazedoxifene hydrochloride (5–20 μM; given overnight) causes human pancreatic cancer cells to undergo apoptosis[2]. IL-6-induced STAT3 nuclear translocation is inhibited by benzedoxifene hydrochloride[2]. By inhibiting GP130, benzedoxifene hydrochloride prevents pancreatic cancer cells from migrating[2].
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| ln Vivo |
In a mouse model, benzodiazepine hydrochloride (5 mg/kg; ir; daily; for 18 days) suppresses the formation 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 # |
198480-56-7
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| Related CAS # |
Bazedoxifene;198481-32-2;Bazedoxifene acetate;198481-33-3
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| SMILES |
CC1=C(C2=CC=C(C=C2)O)N(CC3=CC=C(C=C3)OCCN4CCCCCC4)C5=C1C=C(C=C5)O.Cl
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| Chemical Name |
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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) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| 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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