CI-1040 (PD184352) is a targeted signal transduction inhibitor of MEK with a ki value of 300nM in vitro. CI-1040 (PD184352) is an orally active, highly specific, small-molecule inhibitor of one of the key components of this pathway (MEK1/MEK2), and thereby effectively blocks the phosphorylation of ERK and continued signal transduction through this pathway.
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Source | Antiviral Res (2017). Figure 2. CI-1040 |
| Method | in vitro investigations | |
| Cell Lines | Human lung epithelial cells | |
| Concentrations | 20 μM | |
| Incubation Time | 1 h | |
| Results | This export step is readily blocked in the presence of CI-1040 as evidenced by predominant nuclear staining of the viral NP, the major constituent of the RNPs, as well as the PB1 polymerase, which is associated with RNPs |
| Cell Experiment | |
|---|---|
| Cell lines | CCl39 cells expressing FLAG-ERK5 |
| Preparation method | Cells were serum-starved for 16 h prior to the addition of PD184352, or an equivalent of DMSO vehicle control for 90 min. Single dishes of cells were then stimulated with 10% FBS for 15 min and immune-complex kinase assays performed with either myelin basic protein (MBP; ERK1) or GST-MEF2C (ERK5), as a substrate. PD184352 inhibited FBS-induced ERK1 activation with an IC50 below 1 μM, whereas even a dose of 20 μM PD184352 was insufficient to inhibit ERK5 activity, induced in the same manner and assayed from the same cell extracts as ERK1. |
| Concentrations | 0~1µM |
| Incubation time | 90min |
| Animal Experiment | |
|---|---|
| Animal models | DBA/2-pcy/pcy mice |
| Formulation | DMSO |
| Dosages | 400 mg/kg daily for the first week and then every third day for 6 additional weeks |
| Administration | Oral administration |
| Molecular Weight | 478.67 |
| Formula | C17H14ClF2IN2O2 |
| CAS Number | 212631-79-3 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Neff et al. Laryngoscope. Inhibition of MEK pathway in vestibular schwannoma cell culture.
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