RU-301 是一种泛型TAM抑制剂，能阻断Gas6诱导的TAM激活和致瘤性。RU-301 能显著减少小鼠非酒精性脂肪性肝炎 (NASH) 的纤维化，同时减弱ERK的激活和TGFβ1的表达。RU-301 可用于癌症和非酒精性脂肪性肝炎的研究。
| 生物活性 | RU-301 is a panTAMinhibitor that blocksGas6-inducedTAMactivation and tumorigenicity. RU-301 significantly reduces nonalcoholic steatohepatitis (NASH) fibrosis, along with attenuatesERKactivation andTGFβ1expression. RU-301 can be used in studies ofcancerand nonalcoholic steatohepatitis[1][2]. |
体外研究
(In Vitro) | RU-301 (10 μM; 30 min) inhibits native TAMs activation in H1299 cells[1].
RU-301 (10 μM; 24 h) inhibits migration of H1299 and MDA-MB-231 cells[1].
RU-301 (10 μM; 14 days) inhibits growth of H1299 clonogenic cells under Gas6[1].
Cell Viability Assay[1] | 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.
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Cell Migration Assay[1] | 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[1] | 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
(In Vivo) | RU-301 (100, 300 mg/kg; i.p.; single daily for 4 days) inhibits tumor growth in lung cancer xenograft model[1].
RU-301 (300 mg/kg; i.p.; 3 times a week for 4 weeks) reduces liver fibrosis in mice[2].
| Animal Model: | NOD/SCIDγ mice (4-6 week; lung cancer xenograft model)[1]. | | 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 t1/2life of ~7-8 hours. |
| Animal Model: | WT or Mertk–/–male mice (fed NASH diet for 12 weeks)[2]. | | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(520.33 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.0813 mL | 10.4067 mL | 20.8134 mL | | 5 mM | 0.4163 mL | 2.0813 mL | 4.1627 mL | | 10 mM | 0.2081 mL | 1.0407 mL | 2.0813 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.33 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.33 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 *以上所有助溶剂都可在本网站选购。
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