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RKI-1447 2HCl

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Chemical Structure| 1782109-09-4 同义名 : RKI-1447 dihydrochloride
CAS号 : 1782109-09-4
货号 : A1549873
分子式 : C16H16Cl2N4O2S
纯度 : 98%+
分子量 : 399.295
MDL号 : MFCD28133390
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(125.22 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 RKI-1447 2HCl is a potent, selective ROCK inhibitor with IC50s of 14.5 nM and 6.2 nM for ROCK1 and ROCK2, respectively[1].RKI-1447 2HCl inhibits the growth of colorectal cancer cells and promotes apoptosis[2].At concentrations up to 10 μM, RKI 1447 inhibited the phosphorylation of ROCK substrates MLC-2 and MYPT-1 in human cancer cells, but had no effect on the phosphorylation levels of AKT, MEK and S6 kinases[1].RKI-1447 2HCl significantly inhibited the growth of HCT-8 and HCT-116 cells in the concentration range of 10-320 μM for 24 hours. And in the concentration range of 20-80 μM, RKI-1447 2HCl induced apoptosis in a dose-dependent manner[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.50mL

0.50mL

0.25mL

12.52mL

2.50mL

1.25mL

25.04mL

5.01mL

2.50mL
参考文献

[1]Ronil A Patel, et al. RKI-1447 Is a Potent Inhibitor of the Rho-associated ROCK Kinases With Anti-Invasive and Antitumor Activities in Breast Cancer. Cancer Res. 2012 Oct 1;72(19):5025-34.

[2]Liyi Li, et al. RKI-1447 Suppresses Colorectal Carcinoma Cell Growth via Disrupting Cellular Bioenergetics and Mitochondrial Dynamics. J Cell Physiol. 2020 Jan;235(1):254-266.