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RKI-1447 (dihydrochloride)


CAS No. : 1782109-09-4

1782109-09-4
Price and Availability of CAS No. : 1782109-09-4
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Cat. No. : HY-110339
M.Wt: 399.29
Formula: C16H16Cl2N4O2S
Purity: >98 %
Solubility: DMSO : 50 mg/mL (ultrasonic);H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C)
Introduction of 1782109-09-4 :

RKI 1447 dihydrochloride is a potent and selective ROCK inhibitor with IC50s of 14.5 and 6.2 nM for ROCK1 and ROCK2, respectively[1]. RKI 1447 dihydrochloride suppresses colorectal carcinoma cell growth and promotes apoptosis[2]. 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[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]. In Vivo: 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].

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