| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
The effective inhibition of ROCK2 by ROCK2-IN-10 (compound S9) is due to the interaction of its acetamino side chain with the hydrogen bonds formed by Asp218 and Asn219 in ROCK2[1]. ROCK2-IN-10 (5 μM, 24 h) can disrupt the overall morphology of MDA-MB-231 cells, resulting in blunting of cell pseudopodia and breakage of F-actin stress fibers distributed along the cell contour[1]. ROCK2-IN-10 (2.5-5 μM, 0-48 h) showed a strong and dose-dependent inhibitory effect on cell migration in MDA-MB-231 cells, and showed superior efficacy to Belumosudil at both 24 h and 48 h[1]. ROCK2-IN-10 (2.5-5 μM, 24 h) downregulated the phosphorylation level of STAT3 in a dose-dependent manner, thereby showing a good anti-metastasis effect on MDA-MB-231 cells[1]. ROCK2-IN-10 (72 hours) showed very low cytotoxicity in MDA-MB-231 cells, with an IC50 of 12.77 μM[1].
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|---|---|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: MDA-MB-231 cells Tested Concentrations: 2.5 and 5 μM Incubation Duration: 24 h Experimental Results: Decreased p-STAT3 to nearly half of the control group at the concentration of 5 μM. Reduced p-STAT3 levels in MDA-MB-231 cells in a dose-dependent manner. Cell Migration Assay [1] Cell Types: MDA-MB-231 cells Tested Concentrations: 2.5 and 5 μM Incubation Duration: 0, 24 and 48 h Experimental Results: Inhibited the migration of MDA-MB-231 cells, reducing wound closure to 9.65 % after 24 h, compared to 24.51 % in the control group. Exhibited stronger inhibition than Belumosudil at 5 μM after 24 h, with cell migration rates of 3.48 % compared to 4.74 %. Maintained a more prominent anti-metastatic effect than Belumosudil at 5 μM after 48 h, with cell migration rates of 9.33 % compared to 12.43 %. |
| References |
| Molecular Formula |
C32H38N8O3
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|---|---|
| Molecular Weight |
582.70
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| Appearance |
Typically exists as solids at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7161 mL | 8.5807 mL | 17.1615 mL | |
| 5 mM | 0.3432 mL | 1.7161 mL | 3.4323 mL | |
| 10 mM | 0.1716 mL | 0.8581 mL | 1.7161 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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