RKI-1447 dihydrochloride - CAS:1782109-09-4

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RKI-1447 dihydrochloride

目录号 : KM5463 CAS No. : 1782109-09-4

Data Sheet 产品使用指南

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)。

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500mg	询价	In-stock

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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.

Cell Viability Assay

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

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

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.

分子式

C₁₆H₁₆Cl₂N₄O₂S

分子量

399.29

CAS号

1782109-09-4

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)

溶解性数据

In Vivo:

1.

RKI-1447 dissolved in freshly prepared 20% 2-hydroxypropyl-beta-cyclodextrin (HPCD).

科研文献

•Med Sci Monit. 2020 Feb 6;26:e919220.

Data Sheet

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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