XCT790

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XCT790  纯度: 99.66%

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。

XCT790

XCT790 Chemical Structure

CAS No. : 725247-18-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1207 In-stock
10 mg ￥1097 In-stock
50 mg ￥4259 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

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生物活性

XCT-790 is a potent and selective inverse agonist for ERRα with an IC50 value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ[1][2].

IC50 & Target[1][2]

ERRα

0.37 μM (IC50)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

596.42

Formula

C23H13F9N4O3S
CAS 号

725247-18-7
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
溶解性数据
In Vitro: 

DMSO : 16.67 mg/mL (27.95 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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

*

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Wu F, et al. Estrogen-related receptor alpha (ERRalpha) inverse agonist XCT-790 induces cell death in chemotherapeutic resistant cancer cells. Chem Biol Interact. 2009 Oct 7;181(2):236-42.

    [2]. Kokabu T, et al. Antitumor effect of XCT790, an ERRα inverse agonist, on ERα-negative endometrial cancer cells. Cell Oncol (Dordr). 2019 Apr;42(2):223-235.

    [3]. Busch BB, et al. Identification of a selective inverse agonist for the orphan nuclear receptor estrogen-related receptor alpha. J Med Chem. 2004 Nov 4;47(23):5593-6.

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