XCT790 |
Catalog No.GC10789
One-Click Copy Product Info
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XCT790 is a potent and selective inverse agonist for ERRα with an IC50 value of 0.37μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 725247-18-7
Sample solution is provided at 25 µL, 10mM.
XCT790 is a potent and selective inverse agonist for ERRα with an IC50 value of 0.37μM[1]. Estrogen-related receptor α (ERRα) is a ligand-independent, constitutively active orphan nuclear receptor that, through co-activators like PGC-1α, centrally governs energy metabolism, mitochondrial biogenesis, and tumor progression[2]. XCT790 inhibits ERRα-mediated transcriptional activity by disrupting the interaction between ERRα and its co-activator PGC-1α, and is widely used in studies of metabolic diseases and anti-tumor research[3][4].
In vitro, treatment of HepG2 and multidrug-resistant R-HepG2 cells with XCT790 (0–20μM; 48h) concentration-dependently reduced cell viability, decreased mitochondrial mass by 50%, transiently elevated and then collapsed ΔΨm, quadrupled ROS levels, activated caspases 3/7, 8, and 9, reduced ERR and PGC-1 protein levels， and induced apoptosis in 28.7% of the cells[5]. XCT790(10μM; 24–96h) time-dependently decreases the expression of ERRα, inhibits proliferation, promotes apoptosis in both ERα-positive and -negative endometrial cancer cells[6].
In vivo, XCT790 (2.5mg/kg; i.p.; three times per week for 4 weeks) significantly reduced PaTu8988 xenograft tumor volume by 63% and tumor weight by 62%; when combined with gemcitabine (60mg/kg), XCT790 further downregulated the levels of ERRα, Ki67, and Cyclin D1 while upregulating cleaved-caspase-3 level, inducing G0/G1 cell-cycle arrest and apoptosis in BALB/c nude mice[7].
References:
[1] Busch BB, Stevens WC Jr, Martin R, et al. Identification of a selective inverse agonist for the orphan nuclear receptor estrogen-related receptor alpha. J Med Chem. 2004;47(23):5593-5596.
[2] Tripathi M, Yen PM, Singh BK. Estrogen-Related Receptor Alpha: An Under-Appreciated Potential Target for the Treatment of Metabolic Diseases. Int J Mol Sci. 2020;21(5):1645.
[3] De Luca A, Fiorillo M, Peiris-Pagès M, et al. Mitochondrial biogenesis is required for the anchorage-independent survival and propagation of stem-like cancer cells. Oncotarget. 2015;6(17):14777-14795.
[4] Kokabu T, Mori T, Matsushima H, et al. Antitumor effect of XCT790, an ERRα inverse agonist, on ERα-negative endometrial cancer cells. Cell Oncol (Dordr).
[5] Wu F, Wang J, Wang Y, Kwok TT, Kong SK, Wong C. Estrogen-related receptor alpha (ERRalpha) inverse agonist XCT-790 induces cell death in chemotherapeutic resistant cancer cells.
[6] Sun P, Mao X, Gao M, et al. Novel endocrine therapeutic strategy in endometrial carcinoma targeting estrogen-related receptor α by XCT790 and siRNA. Cancer Manag Res. 2018;10:2521-2535.
[7] Liu SL, Liang HB, Yang ZY, et al. Gemcitabine and XCT790, an ERRα inverse agonist, display a synergistic anticancer effect in pancreatic cancer. Int J Med Sci. 2022;19(2):286-298.
| Cell experiment [1]: | |
Cell lines | HepG2 and R-HepG2 cells |
Preparation Method | HepG2 and R-HepG2 cells were cultured in RPMI 1640 medium with 10% FBS and 100U/ml penicillin–streptomycin. R-HepG2 cells were maintained in culture medium with 1.2μM doxorubicin to keep their MDR properties. All cells were cultured in a humidified atmosphere containing 5% CO2 at 37℃. Cells were seeded in 96-well plates at a density of 2000 cells per well and treated with different concentrations of XCT790 (0–20μM) for 48h with dimethyl sulfoxide as vehicle control. Cell viability was determined by using CellTiter-Glo Luminescent Cell Viability Assay kit and recorded by a VeritasTM Microplate luminometer following technical manuals. Each treatment was performed in triplicate wells per experiment. |
Reaction Conditions | 0–20μM; 48h |
Applications | XCT790 concentration-dependently reduced the viability of Hep2 and multidrug-resistant R-HepG2 cells. |
| Animal experiment [2]: | |
Animal models | BALB/c nude mice |
Preparation Method | PaTu8988 cells (2×106 per mouse) were introduced into the left axilla of BALB/c nude mice (4-week-old, weight 18-22g) through subcutaneous injection. The next day, the animals were stochastically separated into 2 groups of 5: NC group and XCT790 group. The mice were injected with XCT790 (2.5mg/kg) by intraperitoneal injections 3 times a week for 4 weeks, NC group were subjected to DMSO treatment only. Body weight and tumor volume (1/2×length×width2) of mice were monitored weekly. 8 hours posterior to the final treating, the animals were sacrificed, and the tumors were harvested and weighted for further assays. |
Dosage form | 2.5mg/kg; i.p.; three times per week for 4 weeks |
Applications | XCT790 significantly reduced PaTu8988 xenograft tumor volume by 63% and tumor weight by 62%. |
References: | |
| Cas No. | 725247-18-7 | SDF | |
| Chemical Name | (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 | ||
| Canonical SMILES | COC1=C(C=CC(=C1)C=C(C#N)C(=O)NC2=NN=C(S2)C(F)(F)F)OCC3=C(C=C(C=C3)C(F)(F)F)C(F)(F)F | ||
| Formula | C23H13F9N4O3S | M.Wt | 596.42 |
| Solubility | ≥ 14.9mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6767 mL | 8.3834 mL | 16.7667 mL |
| 5 mM | 335.3 μL | 1.6767 mL | 3.3533 mL |
| 10 mM | 167.7 μL | 838.3 μL | 1.6767 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)