220619-73-8

220619-73-8

中文名称220619-73-8
中文同义词化合物 T14145;IRX4204; NRX194204; VTP 194204
英文名称VTP 194204
英文同义词NRX-4204;VTP 194204;NRX 194204;NRX 194204 - NRX 4204/ VTP 194204/ AGN 194204/ AGN 4204;iso IRX-A;2,4-Pentadienoic acid, 3-methyl-5-[(1S,2S)-2-methyl-2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)cyclopropyl]-, (2E,4E)-;IRX-4204;AGN194204,AGN-194204
CAS号220619-73-8
分子式C24H32O2
分子量352.51
EINECS号
相关类别
Mol文件220619-73-8.mol
结构式220619-73-8 结构式

220619-73-8 性质

储存条件Store at -20°C
溶解度溶于二甲基亚砜
形态固体
颜色白色至米白色

220619-73-8 用途与合成方法

AGN194204 (IRX4204) 是一种具有口服活性的,选择性 RXR 激动剂,对 RXRα,RXRβ 和 RXRγ 的 Kd 值分别为 0.4 nM,3.6 nM 和 3.8 nM,EC50 分别为 0.2 nM,0.8 nM 和 0.08 nM。AGN194204 对 RAR 无活性,并具有抗炎和抗癌作用。

RXRα

0.4 nM (Kd)

RXRβ

3.6 nM (Kd)

RXRγ

3.8 nM (Kd)

RXRα

0.2 nM (EC 50 )

RXRβ

0.8 nM (EC 50 )

RXRγ

0.08 nM (EC 50 )

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.
AGN194204 (NRX194204; 1 μM; 72 hours; SK-BR-3 human breast cancer cells) treatment induces apoptosis in breast cancer cells.

Apoptosis Analysis

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

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.

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.

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.

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