PD 325901, Free Base (MEK1/2 Inhibitor III, PD0325901, 391210-10-9), >99%

LC Laboratories' Product Number P-9688 - PD 325901, Free Base (MEK1/2 Inhibitor III, PD0325901, 391210-10-9), >99% - for research use only. PD 325901 is an inhibitor of mitogen activated protein kinase kinase (MEK or MAPKK). The potency, solubility and effectiveness of PD 325901 are greatly improved compared to PD 184352 (CI-1040). PD 325901 potently inhibited the growth of melanoma cells, with and without BRAF mutation. It also had an antiangiogenic activity. The sensitivity of RAS mutant cancers to MEK inhibitors depends on the activity of the phosphatidylinositol 3-kinase (PI3K) pathway. The antiproliferative effect on cancer cells of PD 325901 can be determined by a sensitive imaging biomarker, 3'-deoxy-3'-[18F]fluorothymidine-positron emission tomography ([18F]FLT-PET). PD 325901 potently inhibited the proliferation of thyroid cancer cells with an IC50 of 0.06-0.78 µM. It also has synergistic inhibitory effects when combined with phosphatidylinositol 3-kinase (PI3K) or NF-κB pathway inhibitors in most thyroid cancer cell lines. Blockade of MEK/ERK signaling by PD 325901 greatly enhances the cytotoxicity induced by arsenic trioxide (ATO) through a caspase-dependent mechanism in human myeloma cell lines and in tumor cells from patients with multiple myeloma. A CAS number previously in use for this compound, 870474-62-7, has been deleted by Chemical Abstracts Service.

• Supplier: LC Laboratories
• Product #: P-9688
• Sku #: P-9688_500mg