XCT-790 是ERRα的有效选择性反向激动剂，IC50值为 0.37 μM。XCT-790 在化疗过程中诱导癌细胞死亡。XCT-790 对 ERRγ 和雌激素受体 ERα 和 ERβ 无活性。
| 生物活性 | XCT-790 is a potent and selective inverse agonist forERRαwith anIC50value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistantcancercells. XCT-790 (Compound 12) is inactive againstERRγand the estrogen receptorsERαandERβ[1][2]. |
| IC50& Target[1][2] | |
体外研究
(In Vitro) | XCT-790 (0-40 μM; 48 hours and 72 hours) reduces the viability of MES-SA, MES-SA/DX5, and HepG2 cells in a dose-dependent manner[1].
XCT-790 (10 μM; 24 hours and 48 hours) reduces the protein levels of ERRα in HepG2 and R-HepG2 cell lines after 24 hours and maintains these reduced levels after 48 hours[1].
XCT-790 (10 μM; 48 hours) induces apoptosis in the two cell lines with HepG2 being more sensitive compared to R-HepG2[1].
Cell Viability Assay[1] | Cell Line: | MES-SA, MES-SA/DX5, HepG2 and R-HepG2 cells | | Concentration: | 0 μM, 5 μM, 10 μM, 20 μM, and 40 μM | | Incubation Time: | 48 hours and 72 hours | | Result: | The cells proliferation were decreased in a dose-dependent fashion. |
Western Blot Analysis[1] | Cell Line: | HepG2 and R-HepG2 cells | | Concentration: | 10 μM | | Incubation Time: | 24 hours and 48 hours | | Result: | Reduced the protein levels of ERRα. |
Apoptosis Analysis[1] | Cell Line: | HepG2 and R-HepG2 cells | | Concentration: | 10 μM | | Incubation Time: | 48 hours | | Result: | Induced apoptosis in HepG2 and R-HepG2 cells. |
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体内研究
(In Vivo) | XCT-790 (XCT790; 4 mg/kg; intravenous injection; every three days; for 3 weeks; BALB/c mice) significantly inhibits tumor growth and angiogenesis, and induces apoptosis without a reduction in body weight, in xenograft models[3].
| Animal Model: | Female BALB/c mice (4 weeks of age) with HEC-1A xenograft[3] | | Dosage: | 4 mg/kg | | Administration: | Intravenous injection; every three days; for 3 weeks | | Result: | Suppressed endometrial cancer growth and angiogenesis, and induced apoptosis. |
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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 : 16.67 mg/mL(27.95 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.6767 mL | 8.3834 mL | 16.7667 mL | | 5 mM | 0.3353 mL | 1.6767 mL | 3.3533 mL | | 10 mM | 0.1677 mL | 0.8383 mL | 1.6767 mL |
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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: 1.67 mg/mL (2.80 mM); Suspended solution; Need ultrasonic
此方案可获得 1.67 mg/mL (2.80 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 16.7 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。 *以上所有助溶剂都可在本网站选购。
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