AGN194204 (C09-1102-394)

AGN194204 (IRX4204) is an orally active and selective RXR agonist with K d values 0.4 nM, 3.6 nM and 3.8 nM and EC 50 s of 0.2 nM, 0.8 nM and 0.08 nM for RXRα , RXRβ and RXRγ , respectively. AGN194204 is inactive against RAR. AGN194204 has anti-inflammatory and anticarcinogenic actions.In VitroAGN194204 (NRX194204; 0-100 nM; 24 hours; E, RAW cells) treatment blocks the ability of lipopolysaccharide and tumor necrosis factor-α to induce the release of nitric oxide and interleukin 6 and the degradation of IKBα in RAW264.7 macrophage-like cells. AGN194204 (NRX194204; 1 μM; 72 hours; SK-BR-3 human breast cancer cells) treatment induces apoptosis in breast cancer cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell Line: SK-BR-3 human breast cancer cells Concentration: 1 μM Incubation Time: 72 hours Result: Induced apoptosis in lung and breast cancer cells. Western Blot AnalysisCell Line: E, RAW cells Concentration: 0 nM, 1 nM, 10 nM and 100 nM Incubation Time: 24 hours Result: Blocked the ability of lipopolysaccharide and tumor necrosis factor-α to induce the release of nitric oxide and interleukin 6 and the degradation of IKBα in RAW264.7 macrophage-like cells.In VivoAGN194204 (NRX194204; 30-60 mg/kg; oral administration; daily; for 15 weeks; female A/J mice) treatment significantly reduces the number and size of tumors on the surface of the lungs and reduces the total tumor volume per slide by 64% to 81% compared with the control group . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female A/J mice with vinyl carbamate Dosage: 30 mg/kg, 60 mg/kg Administration: Oral administration; daily; for 15 weeks Result: Significantly reduced the number and size of tumors on the surface of the lungs and reduced the total tumor volume per slide by 64% to 81% compared with the control group.Form:Solid. Specification: ≥99.0% Molecular Formula: C24H32O2 Molecular Weight: 352.51 PubChem CID: 9863341 Isomeric SMILES: C/C(=C/C(=O)O)/C=C/[C@@H]1C[C@]1(C)C2=CC3=C(C=C2)C(CCC3(C)C)(C)C