[CAS NO. 1342278-01-6] RKI-1447
PRODUCTS SPECIFICATIONS [1342278-01-6]
DESCRIPTION [1342278-01-6]
Overview
| MDL | MFCD26142658 |
|---|---|
| Molecular Weight | 326.37 |
| Molecular Formula | C16H14N4O2S |
| SMILES | O=C(NC1=NC(C2=CC=NC=C2)=CS1)NCC3=CC=CC(O)=C3 |
1 Publications Citing Use of MCE
Summary
IC50 & Target
|
ROCK2 6.2 nM (IC 50 ) |
ROCK1 14.5 nM (IC 50 ) |
In Vitro
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 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 is also highly selective at inhibiting ROCK-mediated cytoskeleton re-organization. RKI-1447 inhibits migration, invasion and anchorage-independent tumor growth of breast cancer cells [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
RKI-1447 is highly effective at inhibiting the outgrowth of mammary tumors in a transgenic mouse model. RKI-1447 inhibits mammary tumor growth by 87% and on average the mammary tumors from RKI-1447 treated mice are 7.7 fold smaller compared to those tumors from mice treated with the vehicle control [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 50 mg/mL ( 153.20 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 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 |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.66 mM); Clear solution