PD184161 is a strong and selective inhibitor of MEK-1 and MEK-2 with an IC50 value that ranges from 10-100 nM. 1 More effective at inhibiting phosphorylation of ERK1/2 than the selective MEK inhibitors, PD098059 and U0126. PD184161 is structurally related to clinically-studied MEK inhibitors PD184352 (CI-1040) and PD 325901 and has been shown to inhibit cell proliferation, induce apoptosis, and possess anti-tumor activity in MEK-dependent cancers.

≥98%

store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

PD-184161

white to off-white solid

DMSO : 100 mg/mL (179.35 mM; Need ultrasonic)

Previous study found that PD184161 could inhibit MEK activity in a time- and concentration-dependent manner, which was more effectively than PD098059 or U0126. Moreover, PD184161 could inhibit cell proliferation and induce apoptosis at concentrations of > or = 1.0 μM time- and concentration-dependently.

Animal study showd that tumor xenograft P-ERK levels were significantly reduced 3 to 12 hours after an oral dose of PD184161. Contrarily, tumor xenograft P-ERK levels following long-term treatment of PD184161 were refractory to this signaling effect. PD184161 also significantly suppressed tumor engraftment and initial growth, however, established tumors were not significantly affected. In summary, PD184161 has antitumor effects in HCC in vivo that appear to correlate with suppression of MEK activity.