XCT790
Based on 11 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.67%
- No. CAS: 725247-18-7
- Fòrmula: C23H13F9N4O3S
- Peso molecular:596.42
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Publications Citing Use of MedChemExpress (MCE) XCT790
More- Mol Cancer. 2022 Mar 18;21(1):77. [Abstract]
- Sci Bull. 2025 Sep 29:S2095-9273(25)00984-3. [Abstract]
- Autophagy. 2026 Apr 27. [Abstract]
- Genes Dis. 2020 Dec 23;8(6):891-906. [Abstract]
- J Exp Clin Cancer Res. 2018 Sep 5;37(1):218. [Abstract]
- Cell Rep Med. 2024 Aug 20;5(8):101690. [Abstract]
- Cancer Lett. 2026 May 28:646:218386. [Abstract]
- Cell Death Discov. 2022 Feb 17;8(1):69. [Abstract]
- Oncogene. 2016 Sep 22;35(38):5033-42. [Abstract]
- Mol Med Rep. 2021 Aug;24(2):613. [Abstract]
- bioRxiv. October 20, 2021.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Flow Cytometry
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In Vivo Efficacy Study
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IHC
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WB
Actividad biológica
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ERRα 0.37 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| CV-1 | IC50 |
0.37 μM
Compound: 2, XCT790
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Inverse agonist activity at GAL4-fused ERRalpha (unknown origin) transfected in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay
Inverse agonist activity at GAL4-fused ERRalpha (unknown origin) transfected in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay
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[PMID: 23656512] |
| HEK293 | IC50 |
0.37 μM
Compound: 4, XCT790
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Antagonist activity at ERRalpha LBD expressed in HEK293 cells assessed as Gal4-SRC2 interaction by two hybrid luciferase reporter gene assay
Antagonist activity at ERRalpha LBD expressed in HEK293 cells assessed as Gal4-SRC2 interaction by two hybrid luciferase reporter gene assay
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[PMID: 21218783] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MES-SA, MES-SA/DX5, HepG2 and R-HepG2 cells
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Concentration:0 μM, 5 μM, 10 μM, 20 μM, and 40 μM
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Incubation Time:48 hours and 72 hours
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Result:The cells proliferation were decreased in a dose-dependent fashion.
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Cell Line:HepG2 and R-HepG2 cells
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Concentration:10 μM
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Incubation Time:24 hours and 48 hours
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Result:Reduced the protein levels of ERRα.
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Cell Line:HepG2 and R-HepG2 cells
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Concentration:10 μM
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Incubation Time:48 hours
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Result:Induced apoptosis in HepG2 and R-HepG2 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c mice (4 weeks of age) with HEC-1A xenograft[3]
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Dosage:4 mg/kg
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Administration:Intravenous injection; every three days; for 3 weeks
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Result:Suppressed endometrial cancer growth and angiogenesis, and induced apoptosis.
Chemical Information
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No. CAS 725247-18-7
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Appearance Solid
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Peso molecular 596.42
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Fòrmula C23H13F9N4O3S
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Color Light yellow to yellow
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SMILES
O=C(NC1=NN=C(C(F)(F)F)S1)/C(C#N)=C/C2=CC=C(OCC3=C(C(F)(F)F)C=C(C(F)(F)F)C=C3)C(OC)=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (11)
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Journal Impact Factor
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Most Recent
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Mol Cancer
Cholesterol promotes EGFR-TKIs resistance in NSCLC by inducing EGFR/Src/Erk/SP1 signaling-mediated ERRα re-expression. [Abstract]2022 Mar 18;21(1):77. PMID: 35303882
XCT790 purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2022 Mar 18;21(1):77. [Abstract]
Cells were treated with gefitinib, osimertinib alone or combined with XCT790 (10-20 µM) for 48 h. Then MTT assay was conducted. The results showed that XCT790 sensitized PC-9/GR, H1975 cells to gefitinib and PC-9/OR cells to osimertinib significantly.
XCT790 purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2022 Mar 18;21(1):77. [Abstract]
Cells were cultured in medium with XCT790 for 48 h, then fixed with cold ethanol overnight, incubated with PI/RNase staining buffer for 15 min. Cell cycle distribution was analyzed by flow cytometry.
XCT790 purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2022 Mar 18;21(1):77. [Abstract]
Primary tumor gross appearance tumor weight of the PC-9/GR xenograft after treatment with indicated compounds (XCT790 (8 mg/kg; i.p.; once daily), ect.) for 21 days.
XCT790 purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2022 Mar 18;21(1):77. [Abstract]
XCT790 (8 mg/kg; i.p.; once daily). IHC staining detected Ki67 and ERRα expression in the indicated tumors.
XCT790 purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2022 Mar 18;21(1):77. [Abstract]
XCT790 (8 mg/kg; i.p.; once daily). Western blot assay measured ERRα protein level.
XCT790 purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2022 Mar 18;21(1):77. [Abstract]
XCT790 (8 mg/kg; i.p.; once daily). Cholesterol level in tumor tissue was determined.
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Sci Bull
Nuclear receptor ESRRA promotes ERα-positive breast cancer through dual action on super enhancers and promoters to regulate gene transcriptional programs. [Abstract]2025 Sep 29:S2095-9273(25)00984-3. PMID: 41111053 -
Autophagy
The nuclear receptor ESRRA is a crucial regulator of acute kidney injury through inhibition of the lipophagy-ferroptosis axis. [Abstract]2026 Apr 27. PMID: 42041131 -
Genes Dis
PGC-1α promotes mitochondrial respiration and biogenesis during the differentiation of hiPSCs into cardiomyocytes. [Abstract]2020 Dec 23;8(6):891-906. PMID: 34522716 -
J Exp Clin Cancer Res
ERRα suppression enhances the cytotoxicity of the MEK inhibitor trametinib against colon cancer cells. [Abstract]2018 Sep 5;37(1):218. PMID: 30185207
XCT790 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Sep 5;37(1):218. [Abstract]
The proliferation proteins cMyc and cyclin D1 are identified and confirmed by Western blot analysis after the colon cancer cells are treated with the indicated concentrations of XCT790 (1-5 μM) or DMSO for 48 h.
XCT790 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Sep 5;37(1):218. [Abstract]
Cell proliferation assays at day 3 after the HCT116, SW480 and SW1116 cells were cultured with XCT790 (5 μM and 10 μM) by using the CCK8.
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Cell Rep Med
The SGLT2 inhibitor dapagliflozin ameliorates renal fibrosis in hyperuricemic nephropathy. [Abstract]2024 Aug 20;5(8):101690. PMID: 39168099 -
Cancer Lett
2026 May 28:646:218386. PMID: 41791643 -
Cell Death Discov
Mitochondrial homeostasis regulates definitive endoderm differentiation of human pluripotent stem cells. [Abstract]2022 Feb 17;8(1):69. PMID: 35177589 -
Oncogene
The PLA2R1-JAK2 pathway upregulates ERRα and its mitochondrial program to exert tumor-suppressive action. [Abstract]2016 Sep 22;35(38):5033-42. PMID: 27041564 -
Mol Med Rep
PI3K/AKT phosphorylation activates ERRα by upregulating PGC‑1α and PGC‑1β in gallbladder cancer. [Abstract]2021 Aug;24(2):613. PMID: 34184087 -
Solvente y solubilidad
DMSO : 16.67 mg/mL (27.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 1.67 mg/mL (2.80 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6767 mL | 8.3834 mL | 16.7667 mL | 41.9168 mL |
| 5 mM | 0.3353 mL | 1.6767 mL | 3.3533 mL | 8.3834 mL | |
| 10 mM | 0.1677 mL | 0.8383 mL | 1.6767 mL | 4.1917 mL | |
| 15 mM | 0.1118 mL | 0.5589 mL | 1.1178 mL | 2.7945 mL | |
| 20 mM | 0.0838 mL | 0.4192 mL | 0.8383 mL | 2.0958 mL | |
| 25 mM | 0.0671 mL | 0.3353 mL | 0.6707 mL | 1.6767 mL |
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