Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PD184161 is a novel, orally-active MEK inhibitor. PD184161 inhibited MEK activity (IC50 = 10-100 nM) in a time- and concentration-dependent manner[1].
説明 | PD184161 is a novel, orally-active MEK inhibitor. PD184161 inhibited MEK activity (IC50 = 10-100 nM) in a time- and concentration-dependent manner[1]. |
ターゲット&IC50 | MEK1/2:10-100 nM |
In vitro | 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 | 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]. |
分子量 | 557.56 |
分子式 | C17H13BrClF2IN2O2 |
CAS No. | 212631-67-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (98.64 mM)
You can also refer to dose conversion for different animals. 詳細
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PD184161 212631-67-9 MAPK MEK MAP2K cell Apoptosis neurons Mitogen-activated protein kinase kinase stroke depressive cancer HCC MAPKK Inhibitor PD 184161 inhibit behavioral PD-184161 inhibitor