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CI-1040

CAS No. : 212631-79-3

MCE 站：CI-1040

产品活性：CI-1040 (PD 184352) 是有口服活性，高度特异的 MEK 小分子抑制剂，对 MEK1 的 IC₅₀ 值为 17 nM 。

研究领域：MAPK/ERK Pathway  |  Apoptosis

作用靶点：MEK  |  Apoptosis

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. 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.

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.

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