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RKI-1447 dihydrochloride

产品编号 T61905 CAS 1782109-09-4

RKI 1447 dihydrochloride 是一种有效的，选择性的 ROCK 抑制剂（ROCK1 IC50=14.5 nM，ROCK2 IC50 = 6.2 nM）。RKI 1447 dihydrochloride 对结直肠癌细胞的生长具有抑制作用，并促进其凋亡。

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RKI-1447 dihydrochloride Chemical Structure

RKI-1447 dihydrochloride, CAS 1782109-09-4

规格	价格/CNY		货期	数量
2 mg	￥ 295		5日内发货
5 mg	￥ 595		5日内发货

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RKI-1447 dihydrochloride 的其他形式现货产品:

RKI-1447

其他形式的 RKI-1447 dihydrochloride:

RKI-1447
现货

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生物活性

化学信息

存储 & 溶解度

产品描述	RKI 1447 dihydrochloride is an effective and selective ROCK inhibitor (ROCK1 IC50=14.5 nM, ROCK2 IC50=6.2 nM). RKI 1447 dihydrochloride can inhibit the growth of colorectal cancer cells and promote cell apoptosis.
体外活性	RKI 1447 suppresses phosphorylation of the ROCK substrates MLC-2 and MYPT-1 in human cancer cells, but has no effect on the phosphorylation levels of the AKT, MEK, and S6 kinase at concentrations as high as 10 μM [1]. RKI 1447 (0.003-10 μM) is potent at inhibiting the phosphorylation of the ROCK substrates MLC-2 and MYPT-1 in human cancer cells [1]. RKI 1447 exhibits effective anticancer activity in colorectal carcinoma (CRC). RKI 1447 (10-320 μM; 24 hours) drastically suppresses HCT-8 and HCT-116 cell growth [2]. RKI 1447 (20-80 μM; 24 hours) induces apoptosis in a dose-dependent manner [2]. Cell Viability Assay [2] Cell Line: CRC cell lines HCT-8 and HCT-116 cells Concentration: 0, 10, 20, 40, 80, 160, 320 μM Incubation Time: 24 hours Result: HCT-8 and HCT-116 viability was drastically decreased in a dose-dependent manner. Apoptosis Analysis [2] Cell Line: CRC cell lines HCT-8 and HCT-116 cells Concentration: 0, 20, 40, 80 μM Incubation Time: 24 hours Result: Treatment promoted apoptosis. Western Blot Analysis [1] Cell Line: MDA-MB-231 human breast cancer cells Concentration: 0.003, 0.01, 0.03, 0.1, 0.3, 1, 3,10 μM Incubation Time: Result: Decreased the levels of P-MLC-2, but not total MLC-2, in a concentration-dependent manner with significant effects starting at 100 nM.
体内活性	RKI 1447 (200 mg/kg; i.p. daily for 14 days) inhibits mammary tumor growth in vivo [1]. RKI 1447 (100 mg/kg; i.p.; once every 3 days; for 14 days) exerts antitumor activity on CRC in vivo. RKI 1447 does not exert physiological toxicity on the mice [2]. Animal Model: MMTV/neu transgenic mice [FVB/N-Tg (MMTVneu) 202 Mul/J] [1] Dosage: 200 mg/kg Administration: Treated i.p. daily for 14 days Result: Tumors from mice treated with vehicle increased in size with an average percent change in tumor volume of 68.3%. In contrast, tumors from mice treated with the RKI-1447 increased in size with an average percent change in tumor volume of only 8.8%. Thus, RKI-1447 inhibited mammary tumor growth by 87%. Animal Model: 5-week-old Male BALB/C nude mice [2] Dosage: 100 mg/kg Administration: Intraperitoneally injected; once every 3 days; for 14 days Result: Efficiently blocked CRC tumor growth in vivo.

分子量	399.29
分子式	C16H16Cl2N4O2S
CAS No.	1782109-09-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

计算器

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剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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