| 品牌 | 货号 | 产品规格 | 价格(RMB) | 库存（上海） | 北京 | 武汉 | 南京 | 购买数量 |
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| MedMol | S89032-5mg | 98% | ￥1440.00元 | >10 | - | - | - |
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| MedMol | S89032-25mg | 98% | ￥3600.00元 | 7 | - | - | - |
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| 源叶(MedMol) | S89032-100mg | 98% | ￥10000.00元 | 预计交期：2-3天 | - | - | - |
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| 产品描述： 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 | ||||||||||||||||||||
| 靶点： TAM Receptor;TAMReceptor | ||||||||||||||||||||
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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。 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. |
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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. |
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参考文献： 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. |
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| 溶解性： Soluble in DMSO | ||||||||||||||||||||
| 保存条件： -20℃ | ||||||||||||||||||||
配置溶液浓度参考：
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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