产品
编 号：F741613
分子式：C24H34N2O2
分子量：382.54
分子式：C24H34N2O2
分子量：382.54
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
100mg
询价
询价
结构图
CAS No: 2456434-36-7
产品详情
生物活性：
MSU-42011 is an orally active retinoid X receptor (RXR) agonist. MSU-42011 inhibits the iNOS activity and reduces the expression of p-ERK protein. MSU-42011 has immunomodulatory and antitumor activity.
体内研究：
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。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。MSU42011 (100 mg/kg; PO; 单剂量) 减轻小鼠肺肿瘤模型中的肿瘤负荷。Animal Model:A/J mice (Intraperitoneal injected with the carcinogen ethyl carbamate (0.32 mg/injection) for 8 weeks)
Dosage:25 mg/kg
Administration:Oral administration; One week after, i.p. every other week for a total of 6 injections with Carboplatin (HY-17393) (50 mg/kg) and paclitaxel (15 mg/kg); for 12 weeks
Result:The number and size of detected lung surface tumors increased not in the treatment groupCombines with C/P was most effective in reducing tumor number (67% vs. control), tumor size (76% vs. control), and overall tumor burden (92% vs. control).
Animal Model:A/J lung cancer model (Intraperitoneal injected with the carcinogen ethyl carbamate (0.32 mg/injection) for 8 weeks)
Dosage:100 mg/kg
Administration:Oral administration; After 2 weeks, each mouse was intraperitoneally injected with anti-PD1 and anti-PDL1 antibodies at a rate of 50 μg/mouse, twice a week for a total of 22 times
Result:Showed that an increase in the ratio of anti-tumor CD8 T cells to CD4, CD25 T cells resulted in a significant reduction in tumor volume compared to MSU42011 or anti-PD(L)1 antibody alone.
体外研究：
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。MSU-42011 (300 nM;8 h) 显示在 HepG2 细胞中对 SREBP 的低诱导效果。MSU-42011 (0-5000 nM;24 h) 在 HepG2 细胞中可以激活 RXRα。
MSU-42011 is an orally active retinoid X receptor (RXR) agonist. MSU-42011 inhibits the iNOS activity and reduces the expression of p-ERK protein. MSU-42011 has immunomodulatory and antitumor activity.
体内研究：
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。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。MSU42011 (100 mg/kg; PO; 单剂量) 减轻小鼠肺肿瘤模型中的肿瘤负荷。Animal Model:A/J mice (Intraperitoneal injected with the carcinogen ethyl carbamate (0.32 mg/injection) for 8 weeks)
Dosage:25 mg/kg
Administration:Oral administration; One week after, i.p. every other week for a total of 6 injections with Carboplatin (HY-17393) (50 mg/kg) and paclitaxel (15 mg/kg); for 12 weeks
Result:The number and size of detected lung surface tumors increased not in the treatment groupCombines with C/P was most effective in reducing tumor number (67% vs. control), tumor size (76% vs. control), and overall tumor burden (92% vs. control).
Animal Model:A/J lung cancer model (Intraperitoneal injected with the carcinogen ethyl carbamate (0.32 mg/injection) for 8 weeks)
Dosage:100 mg/kg
Administration:Oral administration; After 2 weeks, each mouse was intraperitoneally injected with anti-PD1 and anti-PDL1 antibodies at a rate of 50 μg/mouse, twice a week for a total of 22 times
Result:Showed that an increase in the ratio of anti-tumor CD8 T cells to CD4, CD25 T cells resulted in a significant reduction in tumor volume compared to MSU42011 or anti-PD(L)1 antibody alone.
体外研究：
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。MSU-42011 (300 nM;8 h) 显示在 HepG2 细胞中对 SREBP 的低诱导效果。MSU-42011 (0-5000 nM;24 h) 在 HepG2 细胞中可以激活 RXRα。
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