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RKI-1447 dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
RKI-1447 dihydrochloride图片
CAS NO:1782109-09-4
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
RKI 1447 dihydrochloride 是一种有效的选择性ROCK抑制剂,对ROCK1ROCK2IC50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 selectiveROCKinhibitor withIC50s of 14.5 and 6.2 nM forROCK1andROCK2, respectively[1]. RKI 1447 dihydrochloride suppresses colorectal carcinoma cell growth and promotesapoptosis[2].

IC50& Target[1][2]

ROCK1

14.5 nM (IC50)

ROCK2

6.2 nM (IC50)

Apoptosis

 

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[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].

Cell Viability Assay[2]

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[2]

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[1]

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[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].

Animal Model:MMTV/neu transgenic mice [FVB/N-Tg (MMTVneu) 202 Mul/J][1]
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[2]
Dosage:100 mg/kg
Administration:Intraperitoneally injected; once every 3 days; for 14 days
Result:Efficiently blocked CRC tumor growth in vivo.
分子量

399.29

性状

Solid

Formula

C16H16Cl2N4O2S

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 Vitro: 

DMSO : 50 mg/mL(125.22 mM;Need ultrasonic)

H2O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.5044 mL12.5222 mL25.0445 mL
5 mM0.5009 mL2.5044 mL5.0089 mL
10 mM0.2504 mL1.2522 mL2.5044 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 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-CDin 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 μL20% 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。

*以上所有助溶剂都可在本网站选购。