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| 25mg |
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Purity: ≥98%
RKI-1447 (ROCK Inhibitor XIII; RKI 1447; RKI1447) is a potent small molecule inhibitor of ROCK1 and ROCK2 with potential antitumor activities against breast cancer. It inhibits ROCK1 and ROCK2 with IC50s of 14.5 nM and 6.2 nM, respectively. RKI-1447 is a Type I kinase inhibitor that binds the ATP binding site through interactions with the hinge region and the DFG motif. RKI-1447 suppressed phosphorylation of the ROCK substrates MLC-2 and MYPT-1 in human cancer cells.
| ln Vitro |
RKI-1447 is a Type I kinase inhibitor that interacts with the hinge region and DFG motif to bind the ATP binding site. While AKT, MEK, and S6 kinase phosphorylation levels remain unaffected by RKI-1447 at concentrations up to 10 μM, it decreases phosphorylation of the ROCK substrates mLC-2 and MYPT-1 in human cancer cells. Inhibiting ROCK-mediated cytoskeleton reorganization is another highly selective action of RKI-1447. Breast cancer cells' ability to migrate, invade, and develop tumors without anchorage is inhibited by RKI-1447[1].
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| ln Vivo |
In a transgenic mouse model, RKI-1447 is very successful in preventing the formation of mammary cancers. RKI-1447 suppresses the growth of mammary tumors by 87%, and on average, the tumors from mice treated with RKI-1447 are 7.7 times smaller than those from animals given with vehicle control[1].
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| References |
| Molecular Formula |
C16H14N4O2S
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| Molecular Weight |
326.37
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| Exact Mass |
326.083
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| CAS # |
1342278-01-6
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| Related CAS # |
1782109-09-4
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| PubChem CID |
60138149
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.701
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| LogP |
1.42
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
23
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| Complexity |
392
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GDVRVPIXWXOKQO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H14N4O2S/c21-13-3-1-2-11(8-13)9-18-15(22)20-16-19-14(10-23-16)12-4-6-17-7-5-12/h1-8,10,21H,9H2,(H2,18,19,20,22)
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| Chemical Name |
1-[(3-hydroxyphenyl)methyl]-3-(4-pyridin-4-yl-1,3-thiazol-2-yl)urea
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.66 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 15% Captisol:15 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0640 mL | 15.3200 mL | 30.6401 mL | |
| 5 mM | 0.6128 mL | 3.0640 mL | 6.1280 mL | |
| 10 mM | 0.3064 mL | 1.5320 mL | 3.0640 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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