PD-325901, Free Base (PD 0325901, MEK1/2 Inhibitor III)

A selective and ATP non-competitive MEK inhibitor that suppresses the phosphorylation of ERK in murine colon 26 tumors (IC50 = 0.33nM). In combination with the GSK-3 inhibitor CHIR99021, prevents cell differentiation and sustains self-renewal of embryonic stem (ES) cells.

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- B 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.

Small volumes of PD-325901, Free Base biochemical vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

MBS6061791 is a biochemical targeting PD-325901, Free Base. Also known as PD-325901, Free Base (PD 0325901, MEK1/2 Inhibitor III).