产品
编 号:F038363
分子式:C21H19F3N4O4S
分子量:480.46
产品类型
结构图
CAS No: 1110873-99-8
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产品详情
生物活性:
RU-301 is a pan TAM inhibitor that blocks Gas6-induced TAM activation and tumorigenicity. RU-301 significantly reduces nonalcoholic steatohepatitis (NASH) fibrosis, along with attenuates ERK activation and TGFβ1 expression. RU-301 can be used in studies of cancer and nonalcoholic steatohepatitis.
体内研究:
RU-301 (100、300 mg/kg;腹腔注射;每天一次,持续 4 天) 抑制肺癌异种移植模型中的肿瘤生长。 RU-301 (300 mg/kg;腹腔注射;每周 3 次,持续 4 周) 减少小鼠的肝纤维化。Animal Model:NOD/SCIDγ mice (4-6 week; lung cancer xenograft model).
Dosage:100, 300 mg/kg
Administration:Intraperitoneal injection; single daily for 4 days
Result:Significantly decreased tumor volume while body weights were not significantly different.Showed no notable toxicity but displayed good bioavailability with a t1/2 life of ~7-8 hours.
Animal Model:WT or Mertk?/? male mice (fed NASH diet for 12 weeks).
Dosage:300 mg/kg
Administration:Intraperitoneal injection; 3 times a week for 4 weeks
Result:Reduced liver fibrosis as indicated by decreases in liver picrosirius red staining and collagen gene expression.
体外研究:
RU-301 (10 μM;30 分钟) 抑制 H1299 细胞中的天然 TAM 激活。 RU-301 (10 μM;24 小时) 抑制 H1299 和 MDA-MB-231 细胞的迁移。 RU-301 (10 μM;14 天) 在 Gas6 下抑制 H1299 克隆形成细胞的生长。