RU-301|cas:1110873-99-8|西域试剂

RU-301,99.44%

产品编号：Bellancom-119039| CAS NO：1110873-99-8| 分子式：C₂₁H₁₉F₃N₄O₄S| 分子量：480.46

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货号	价格	库存与货期
Bellancom-119039	￥3100.00	杭州北京（现货）
Bellancom-119039	￥4900.00	杭州北京（现货）
Bellancom-119039	￥8900.00	杭州北京（现货）
Bellancom-119039	￥14000.00	杭州北京（现货）

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RU-301

产品介绍

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 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.

体外研究

RU-301 (10 μM; 30 min) inhibits native TAMs activation in H1299 cells.
RU-301 (10 μM; 24 h) inhibits migration of H1299 and MDA-MB-231 cells.
RU-301 (10 μM; 14 days) inhibits growth of H1299 clonogenic cells under Gas6.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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.
RU-301 (300 mg/kg; i.p.; 3 times a week for 4 weeks) reduces liver fibrosis in mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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 t_1/2 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.

体内研究

RU-301 (100, 300 mg/kg; i.p.; single daily for 4 days) inhibits tumor growth in lung cancer xenograft model.
RU-301 (300 mg/kg; i.p.; 3 times a week for 4 weeks) reduces liver fibrosis in mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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 t_1/2 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.

体内研究

RU-301 (100, 300 mg/kg; i.p.; single daily for 4 days) inhibits tumor growth in lung cancer xenograft model.
RU-301 (300 mg/kg; i.p.; 3 times a week for 4 weeks) reduces liver fibrosis in mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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 t_1/2 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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (520.33 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液