RKI-1447 dihydrochloride|1782109-09-4|-陌孚医药/Medlife

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RKI-1447 dihydrochloride

目录号: PL11050 纯度: ≥98%

CAS No. :1782109-09-4

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中文名称	RKI-1447 dihydrochloride
英文名称	RKI-1447 dihydrochloride
英文别名	RKI 1447 (dihydrochloride);RKI 1447 dihydrochloride;1-[(3-hydroxyphenyl)methyl]-3-(4-pyridin-4-yl-1,3-thiazol-2-yl)urea;dihydrochloride;N-[(3-Hydroxyphenyl)methyl]-N'-[4-(4-pyridinyl)-2-thiazolyl]urea dihydrochloride;RKI-1447 dihydrochloride
Cas No.	1782109-09-4
分子式	C₁₆H₁₆Cl₂N₄O₂S
分子量	399.29
包装储存	4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

产品详情	RKI 1447 dihydrochloride 是一种有效的选择性 ROCK 抑制剂，对 ROCK1 和 ROCK2 的 IC₅₀ 分别为 14.5 和 6.2 nM。RKI 1447 dihydrochloride 抑制结直肠癌细胞的生长并促进细胞凋亡 (apoptosis)。
生物活性	RKI 1447 dihydrochloride is a potent and selective ROCK inhibitor with IC 50 s of 14.5 and 6.2 nM for ROCK1 and ROCK2, respectively. RKI 1447 dihydrochloride suppresses colorectal carcinoma cell growth and promotes apoptosis.
性状	Solid
IC50 & Target[1][2]	ROCK1 14.5 nM (IC50) ROCK2 6.2 nM (IC
体外研究(In Vitro)	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. 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. 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. RKI 1447 (20-80 μM; 24 hours) induces apoptosis in a dose-dependent manner. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	RKI 1447 (200 mg/kg; i.p. daily for 14 days) inhibits mammary tumor growth in vivo. 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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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.

溶解度数据	In Vitro: DMSO : 50 mg/mL (125.22 mM; Need ultrasonic)H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)配制储备液

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