Bazedoxifene (TSE-424) 是一种有口服活性的，能透过血脑屏障的，非甾体、选择性的雌激素受体调节剂 (SERM)，对 ERα 和 ERβ 作用的IC50值分别为 26 nM 和 99 nM，可用于骨质疏松症的研究。Bazedoxifene 也是一种IL-6/GP130蛋白相互作用抑制剂，可用于胰腺癌的研究。
| 生物活性 | Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidalselectiveestrogen receptor modulator(SERM), withIC50s of 23 nM and 99 nM forERαandERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor ofIL-6/GP130protein-protein interactions and can be used for the research of pancreaticcancer[1][2]. |
| IC50& Target | IC50: 26 nM (ERα), 99 nM (ERβ)[1] |
体外研究
(In Vitro) | Bazedoxifene is a small molecular GP130 inhibitor, which binds to GP130 D1 domain[1].
Bazedoxifene inhibits STAT3 phosphorylation induced by Il-6 and IL-11 in GP130/STAT3 pathway signaling[1].
Bazedoxifene (10 μM-20 μM; 2 hours) inhibits STAT3 Phosphorylation Induced by cytokines in human pancreatic cancer cells[2].
Bazedoxifene (5-20 μM; overnight) induces apoptosis in human pancreatic cancer cells[2].
Bazedoxifene inhibits STAT3 nuclear translocation induced by IL-6[2].
Bazedoxifene blocks the cells migration in pancreatic cancer cells by inhibition of GP130[2].
Western Blot Analysis[2] | Cell Line: | AsPC-1 cells | | Concentration: | 10 μM, 20 μM | | Incubation Time: | 2 hours | | Result: | Inhibited IL-6, IL-11 or OSM (50 ng/mL) induced STAT3 phosphorylation. |
Apoptosis Analysis[2] | Cell Line: | Capan-1 cells, BxPC-3 cells, HPAF-II cells, HPAC cells | | Concentration: | 10 μM, 20 μM (Capan-1); 5 μM, 10 μM (BxPC-3); 10 μM, 20 μM (HPAF-II); 10 μM, 15 μM (HPAC) | | Incubation Time: | Overnight | | Result: | Induced apoptosis. |
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体内研究
(In Vivo) | Bazedoxifene (5 mg/kg; i.g.; daily, for 18 days) inhibits Capan-1 tumor growth in mouse model in vivo[2].
| Animal Model: | 6-week-old female athymic nude mice[2] | | Dosage: | 5 mg/kg | | Administration: | Oral gavage, daily, for 18 days | | Result: | Suppressed pancreatic cancer xenograft tumor growth and induced apoptosis in tumor cells. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(212.49 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.1249 mL | 10.6247 mL | 21.2495 mL | | 5 mM | 0.4250 mL | 2.1249 mL | 4.2499 mL | | 10 mM | 0.2125 mL | 1.0625 mL | 2.1249 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.31 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.31 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (5.31 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.31 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.31 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.31 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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