PD 184161 是一种口服有效的，时间和浓度依赖的MEK抑制剂，IC50为10-100 nM。它诱导抑郁样行为，抑制细胞增殖并诱导细胞凋亡。

PD184161 is a novel, orally-active MEK inhibitor. PD184161 inhibited MEK activity (IC50 = 10-100 nM) in a time- and concentration-dependent manner[1].

PD184161 inhibited MEK activity (IC50 = 10-100 nM) in a time- and concentration-dependent manner more effectively than PD098059 or U0126. PD184161 inhibited cell proliferation and induced apoptosis at concentrations of >or = 1.0 microM in a time- and concentration-dependent manner[1].

In vivo, tumor xenograft P-ERK levels were significantly reduced 3 to 12 hours after an oral dose of PD184161 (P< .05). Contrarily, tumor xenograft P-ERK levels following long-term (24 days) daily dosing of PD184161 were refractory to this signaling effect. PD184161 significantly suppressed tumor engraftment and initial growth (P< .0001); however, established tumors were not significantly affected. In conclusion, PD184161 has antitumor effects in HCC in vivo that appear to correlate with suppression of MEK activity [1].

212631-67-9

C17H13BrClF2IN2O2

557.56

DMSO:29 mg/mL (52.00 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years