MSU-42011

CAS: 2456434-36-7 F: C24H34N2O2 W: 382.54

MSU-42011 is an orally active retinoid X receptor (RXR) agonist. MSU-42011 inhibits the expression of iNOS and p-ERK pro

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Bioactivity	MSU-42011 is an orally active retinoid X receptor (RXR) agonist. MSU-42011 inhibits the expression of iNOS and p-ERK protein. MSU-42011 has immunomodulatory and antitumor activity. MSU-42011 can be used for cancer research[1].
Invitro	MSU-42011 (0-1 μM) 在 RAW264.7 巨噬细胞样细胞中抑制 iNOS 的IC50 值为 158 nM[1]。MSU-42011 (300 nM;8 h) 显示在 HepG2 细胞中对 SREBP 的低诱导效果[1]。MSU-42011 (0-5000 nM;24 h) 在 HepG2 细胞中可以激活 RXRα[1]。 RT-PCR[1] Cell Line:
In Vivo	MSU-42011 (25 mg/kg, 口服, 持续 12 周) 显著降低了 A/J 小鼠肺癌模型中肿瘤的数量、大小和总体肿瘤负荷。与对照组相比，增殖活跃的细胞较少，并显示 p-ERK 显著降低[1]。MSU-42011 (25 mg/kg; 口服; 单剂量) 在 A/J 小鼠肺癌模型中与 C/P 联合用药，在减少肿瘤数量、肿瘤大小和总体肿瘤负荷方面最有效。减少了肺中的巨噬细胞，增加了 CD8+T 细胞的活化标志物[1]。MSU42011 (100 mg/kg; PO; 单剂量) 减轻小鼠肺肿瘤模型中的肿瘤负荷[2]。 Animal Model:
Name	MSU-42011
CAS	2456434-36-7
Formula	C24H34N2O2
Molar Mass	382.54
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Moerland JA, et al. The novel rexinoid MSU-42011 is effective for the treatment of preclinical Kras-driven lung cancer. Sci Rep. 2020 Dec 17;10(1):22244. [2]. Leal AS, et al. The RXR Agonist MSU42011 Is Effective for the Treatment of Preclinical HER2+ Breast Cancer and Kras-Driven Lung Cancer. Cancers (Basel). 2021 Oct 6;13(19):5004.