220619-73-8
220619-73-8 structure
- Name: AGN194204
- Chemical Name: (2E,4E)-3-Methyl-5-[(1S,2S)-2-methyl-2-(5,5,8,8-tetramethyl-5,6,7 ,8-tetrahydro-2-naphthalenyl)cyclopropyl]-2,4-pentadienoic acid
- CAS Number: 220619-73-8
- Molecular Formula: C24H32O2
- Molecular Weight: 352.51000
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2016-02-16 16:06:25
- Modify Date: 2024-01-10 20:34:21
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AGN194204 (IRX4204) is an orally active and selective RXR agonist with Kd values 0.4 nM, 3.6 nM and 3.8 nM and EC50s 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[1][2].
| Name | (2E,4E)-3-Methyl-5-[(1S,2S)-2-methyl-2-(5,5,8,8-tetramethyl-5,6,7 ,8-tetrahydro-2-naphthalenyl)cyclopropyl]-2,4-pentadienoic acid |
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| Description | AGN194204 (IRX4204) is an orally active and selective RXR agonist with Kd values 0.4 nM, 3.6 nM and 3.8 nM and EC50s 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[1][2]. |
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| Related Catalog | |
| Target |
RXRα:0.4 nM (Kd) RXRβ:3.6 nM (Kd) RXRγ:3.8 nM (Kd) RXRα:0.2 nM (EC50) RXRβ:0.8 nM (EC50) RXRγ:0.08 nM (EC50) |
| In Vitro | AGN194204 (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[1]. AGN194204 (NRX194204; 1 μM; 72 hours; SK-BR-3 human breast cancer cells) treatment induces apoptosis in breast cancer cells[1]. Apoptosis Analysis[1] Cell 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 Analysis[1] Cell 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 Vivo | AGN194204 (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[1]. Animal Model: Female A/J mice with vinyl carbamate[1] 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. |
| References |
| Molecular Formula | C24H32O2 |
|---|---|
| Molecular Weight | 352.51000 |
| Exact Mass | 352.24000 |
| PSA | 37.30000 |
| LogP | 5.90030 |