| 產品描述： | 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 |
| 靶點： |
TAM Receptor;TAMReceptor |
| 體外研究： |
RU-301 (10 μM；30 分鐘) 抑制 H1299 細胞中的天然 TAM 激活。 RU-301 (10 μM；24 小時) 抑制 H1299 和 MDA-MB-231 細胞的遷移。 RU-301 (10 μM；14 天) 在 Gas6 下抑制 H1299 克隆形成細胞的生長。 Cell Viability Assay Cell Line: H1299, MDA-MB-231 cells Concentration: 10 μM (for H1299); 2.5, 5 μM (for MDA-MB-231) Incubation Time: 30 min (pre-incubate) Result: Suppressed Gas6-inducible native phosphorylation of native Axl.Partially blocked Gas6-induced activation of Akt and Erk in H1299 or MDA-MB-231 at 5 μM.Inhibited the Gas6-induced phosphorylation of not only native Axl but also native Tyro3 and MerTK in H1299 at 10 μM. Cell Migration Assay Cell Line: H1299, MDA-MB-231 cells Concentration: 10 μM Incubation Time: 24 h Result: Strongly suppressed Gas6-inducible motility of H1299 lung cancer cell line. Cell Viability Assay Cell Line: H1299 cells Concentration: 10 μM Incubation Time: 14 days Result: Suppressed clonogenic growth of H1299 cells when cultured in the presence of Gas6. |
| 體內研究： |
RU-301 (100、300 mg/kg；腹腔注射；每天一次，持續 4 天) 抑制肺癌異種移植模型中的腫瘤生長。 RU-301 (300 mg/kg；腹腔注射；每周 3 次，持續 4 周) 減少小鼠的肝纖維化。 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. |
| 參考文獻： |
1. Kimani SG, et al. Small molecule inhibitors block Gas6-inducible TAM activation and tumorigenicity. Sci Rep. 2017 Mar 8;7:43908. 2. Cai B, et al. Macrophage MerTK Promotes Liver Fibrosis in Nonalcoholic Steatohepatitis. Cell Metab. 2020 Feb 4;31(2):406-421.e7. |
| 溶解性： |
Soluble in DMSO |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.081 ml |
10.407 ml |
20.813 ml |
| 5 mM |
0.416 ml |
2.081 ml |
4.163 ml |
| 10 mM |
0.208 ml |
1.041 ml |
2.081 ml |
| 50 mM |
0.042 ml |
0.208 ml |
0.416 ml |
|
| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經營許可證（不帶存儲）
營業執照(三證合一)
北京