RKI-1447 dihydrochloride|cas:1782109-09-4|西域试剂

RKI-1447 dihydrochloride,98.04%

产品编号：Bellancom-110339| CAS NO：1782109-09-4| 分子式：C₁₆H₁₆Cl₂N₄O₂S| 分子量：399.29

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-110339	￥600.00	杭州北京（现货）
Bellancom-110339	￥1100.00	杭州北京（现货）
Bellancom-110339	￥2400.00	杭州北京（现货）
Bellancom-110339	￥4000.00	杭州北京（现货）
Bellancom-110339	￥6400.00	杭州北京（现货）

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RKI-1447 dihydrochloride

产品介绍

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 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
(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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

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

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5044 mL	12.5222 mL	25.0445 mL
5 mM	0.5009 mL	2.5044 mL	5.0089 mL
10 mM	0.2504 mL	1.2522 mL	2.5044 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.26 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.26 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.26 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。