XCT790

SKU: orb1224136

Description

A potent and selective ERRα inverse agonist with IC50 of 300-500 nM in transient transfection assays; shows no significant antagonist activity on related nuclear receptors (ERRγ or ERα, LXRα, LXRβ, FXR, PPARα, PPARδ, PPARγ, Nurr1, RARα, RORα, and RXRα) at 10 uM; inhibits PGC-1α regulation of ERRα and ERRα target gene expression; inhibits proliferation in cellular models of breast cancer.(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.(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.

Key Properties

• CAS Number: 725247-18-7
• MW: 596.4249
• Purity: >98% (HPLC)
• Formula: C₂₃H₁₃F₉N₄O₃S
• SMILES: O=C(NC1=NN=C(C(F)(F)F)S1)/C(C#N)=C/C2=CC=C(OCC3=CC=C(C(F)(F)F)C=C3C(F)(F)F)C(OC)=C2
• Target: Estrogen Receptor/ERR
• Solubility: DMSO: 21 mg/mL

Bioactivity

• 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. 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.
• 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. 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

XCT 790 | XCT-790

Quick Database Links

Gene Symbol

Estrogen Receptor/ERR