产品
编 号：F622126
分子式：C16H16Cl2N4O2S
分子量：399.29
分子式：C16H16Cl2N4O2S
分子量：399.29
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
100mg
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结构图
CAS No: 1782109-09-4
产品详情
生物活性：
RKI 1447 dihydrochloride is a potent and selective ROCK inhibitor with IC50s of 14.5 and 6.2 nM for ROCK1 and ROCK2, respectively. RKI 1447 dihydrochloride suppresses colorectal carcinoma cell growth and promotes apoptosis.
体内研究：
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.Animal Model:MMTV/neu transgenic mice [FVB/N-Tg (MMTVneu) 202 Mul/J]
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
Dosage:100 mg/kg
Administration:Intraperitoneally injected; once every 3 days; for 14 days
Result:Efficiently blocked CRC tumor growth in vivo.
体外研究：
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.
RKI 1447 dihydrochloride is a potent and selective ROCK inhibitor with IC50s of 14.5 and 6.2 nM for ROCK1 and ROCK2, respectively. RKI 1447 dihydrochloride suppresses colorectal carcinoma cell growth and promotes apoptosis.
体内研究：
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.Animal Model:MMTV/neu transgenic mice [FVB/N-Tg (MMTVneu) 202 Mul/J]
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
Dosage:100 mg/kg
Administration:Intraperitoneally injected; once every 3 days; for 14 days
Result:Efficiently blocked CRC tumor growth in vivo.
体外研究：
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.
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