Network Version
CI-1040 Data Sheet
| Product Name: | CI-1040 |
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|---|---|---|
| CAS No.: | 212631-79-3 | |
| Cat. No.: | HY-50295 | |
| MWt: | 478.66 | |
| Formula: | C17H14ClF2IN2O2 | |
| Purity : | >98% | |
| Solubility: | DMSO : ≥ 100 mg/mL | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
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CI-1040 (PD 184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1.
IC50 & Target:IC50: 17 nM (MEK)[1]
In Vitro: CI-1040 directly inhibits MEK1 with an IC50 of 17 nM. It has also been shown to have little activity against a panel of related kinases with IC50 values more than 2.5 orders of magnitude higher. Treatment of whole cells with CI-1040 completely inhibits the mitogen-stimulated phosphorylation of ERK. CI-1040 at a concentration of 1 μM is found to inhibit phosphorylation of ERK1 and ERK2 by 99% and 92%, respectively in MDA-MB-231 breast cancer cells[1]. CI-1040 induces apoptosis and inhibits proliferation in U-937 cells in a dose and time-dependent manner. CI-1040 induces a significant increase in PUMA mRNA and protein levels[2]. In Vivo: The systemic administration of the MEK inhibitor CI-1040 reduces adenoma formation to a third and significantly restores lung structure. The proliferation rate of lung cells of mice treated with CL-1040 is decreased without any obvious effects on differentiation of pneumocytes[3]. |
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