XCT790|725247-18-7|-陌孚医药/Medlife

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XCT790

目录号: PC10473 纯度: ≥98%

CAS No. :725247-18-7

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PC10473-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥1274.00	请登录

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中文名称

XCT790

中文别名

3-[4-[[2,4-二(三氟甲基)苄基]氧基]-3-甲氧基苯基]-2-氰基-N-(5-三氟甲基-[1,3,4]噻二唑-2-基)丙烯酰胺;XCT790 抑制剂

英文名称

XCT790

英文别名

XCT 790;(E)-3-[4-[[2,4-bis(trifluoromethyl)phenyl]methoxy]-3-methoxyphenyl]-2-cyano-N-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]prop-2-enamide;HMS3263N08;XCT-790;3-[4-(2,4-Bis-trifluoromethylbenzyloxy)-3-methoxyphenyl]-2-cyano-N-(5-trifluoromethyl-1,3,4-thiadiazol-2-yl)acrylamide;XCT790

Cas No.

725247-18-7

分子式

C₂₃H₁₃N₄O₃F₉S

分子量

596.42

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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.

性状

Solid

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.
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.
XCT-790 (10 μM; 48 hours) induces apoptosis in the two cell lines with HepG2 being more sensitive compared to R-HepG2.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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

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

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.

Medlife 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
Dosage:	4 mg/kg
Administration:	Intravenous injection; every three days; for 3 weeks
Result:	Suppressed endometrial cancer growth and angiogenesis, and induced apoptosis.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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. [Information]

[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. [Information]

[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. [Information]

溶解度数据

体外研究:

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

配制储备溶液

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 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 ddH?O 中，得到澄清透明的生理盐水溶液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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