RKI-1447 dihydrochloride

Name: RKI-1447 dihydrochloride
Brand: MedChemExpress
SKU: HY-110339
Rating: 4.5 (3 reviews)

Cat. No.: HY-110339 Purity: 98.04%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

RKI-1447 dihydrochloride Chemical Structure

CAS No. : 1782109-09-4

Size	Price	Stock	Quantity
5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 640	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 3 publication(s) in Google Scholar

Other Forms of RKI-1447 dihydrochloride:

RKI-1447 In-stock

2 Publications Citing Use of MCE RKI-1447 dihydrochloride

: RKI-1447 dihydrochloride purchased from MedChemExpress. Usage Cited in: Med Sci Monit. 2020 Feb 6;26:e919220. [Abstract]; The effects of RKI-1447 on glucose tolerance and insulin resistance in a mouse model of nonalcoholic fatty liver disease (NAFLD) induced by a high-fat diet. The expression of the insulin receptor substrate-1 (IRS1) are shown. The mice were fed with a high-fat diet for 12 weeks. From the ninth week, the mice were treated orally with the ROCK inhibitor RKI-1447 (2 mg/kg to 8 mg/kg) twice weekly for three weeks.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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].

IC₅₀ & Target^[1]^[2]

ROCK1

14.5 nM (IC₅₀)

ROCK2

6.2 nM (IC₅₀)

Apoptosis

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

MedChemExpress (MCE) 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]^[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.

Molecular Weight

399.29

Formula

C₁₆H₁₆Cl₂N₄O₂S

CAS No.

1782109-09-4

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(NC1=NC(C2=CC=NC=C2)=CS1)NCC3=CC=CC(O)=C3.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (125.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.04%

Select Batch:

Data Sheet (278 KB) SDS (252 KB)

COA (247 KB) HNMR (338 KB) LCMS (121 KB)

Handling Instructions (2659 KB)

References

[1]. Ronil A Patel, et al. RKI-1447 Is a Potent Inhibitor of the Rho-associated ROCK Kinases With Anti-Invasive and Antitumor Activities in Breast Cancer. Cancer Res. 2012 Oct 1;72(19):5025-34. [Content Brief]

[2]. Liyi Li, et al. RKI-1447 Suppresses Colorectal Carcinoma Cell Growth via Disrupting Cellular Bioenergetics and Mitochondrial Dynamics. J Cell Physiol. 2020 Jan;235(1):254-266. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5044 mL	12.5222 mL	25.0445 mL	62.6111 mL
	5 mM	0.5009 mL	2.5044 mL	5.0089 mL	12.5222 mL
	10 mM	0.2504 mL	1.2522 mL	2.5044 mL	6.2611 mL
	15 mM	0.1670 mL	0.8348 mL	1.6696 mL	4.1741 mL
	20 mM	0.1252 mL	0.6261 mL	1.2522 mL	3.1306 mL
	25 mM	0.1002 mL	0.5009 mL	1.0018 mL	2.5044 mL
	30 mM	0.0835 mL	0.4174 mL	0.8348 mL	2.0870 mL
	40 mM	0.0626 mL	0.3131 mL	0.6261 mL	1.5653 mL
	50 mM	0.0501 mL	0.2504 mL	0.5009 mL	1.2522 mL
	60 mM	0.0417 mL	0.2087 mL	0.4174 mL	1.0435 mL
	80 mM	0.0313 mL	0.1565 mL	0.3131 mL	0.7826 mL
	100 mM	0.0250 mL	0.1252 mL	0.2504 mL	0.6261 mL