PD184161_product_DataBase

Bioactivity	PD184161 is an orally active MEK inhibitor. PD184161 inhibits MEK activity (IC50=10-100 nM) in a time- and concentration-dependent manner. PD184161 inhibits cell proliferation and induces apoptosis. PD184161 produces depressive-like behavior[1][2].
Invitro	PD184161 (1-20 μM; 24, 48, or 72 hours) inhibits cell proliferation and induces apoptosis in a time and concentration dependent manner[1].PD184161 (0.1 and 1.0 μM; 1 hour) inhibits ERK1,2 phosphorylation[1].PD184161 (5 μM; 30 min) prevents the toxic effects of bicuculline[3]. Cell Proliferation Assay[1] Cell Line:
In Vivo	PD184161 reduces tumor xenograft P-ERK levels in 3-12 hours after an oral dose[1].PD184161 (300 mg/kg; orogastric gavage twice daily for 38 days) significantly suppresses tumor engraftment and initial growth[1].PD184161 (30 mg/kg; i.p.; single injection) produces depressive-like behavior[2].PD184161 (500 μg/kg; intravenous injection) prevents the progression of neurological deficits and brain damage after stroke[3]. Animal Model:
Name	PD184161
CAS	212631-67-9
Formula	C17H13BrClF2IN2O2
Molar Mass	557.56
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Reference	[1]. Klein PJ, et al. The effects of a novel MEK inhibitor PD184161 on MEK-ERK signaling and growth in human liver cancer. Neoplasia. 2006 Jan;8(1):1-8. [2]. Duman CH, et al. A role for MAP kinase signaling in behavioral models of depression and antidepressant treatment. Biol Psychiatry. 2007 Mar 1;61(5):661-70. [3]. Gladbach A, et al. ERK inhibition with PD184161 mitigates brain damage in a mouse model of stroke. J Neural Transm (Vienna). 2014 May;121(5):543-7.

PeptideDB

PD184161

CAS: 212631-67-9 F: C17H13BrClF2IN2O2 W: 557.56