109511-58-2

Solubility:DMSO

Storage:at -20℃ 2 years

Biologieal

PD0325901 is non-competitive with ATP and is exquisitely specific and highly potent against purified MEK, exhibiting a Ki^app of 1 nM against activated MEK1 and MEK2. PD0325901 is roughly 500-fold more potent than CI-1040 with respect to its cellular effects on phosphorylation of ERK1 and ERK2, exhibiting subnanomolar activity.
A single oral dose of PD0325901 (25 mg/kg) suppressed phosphorylation of ERK by >50% at 24 hours post-dosing.
Anticancer activity of PD 0325901 has been demonstrated for a broad spectrum of human tumor xenografts, significantly inhibiting the growth of 6 out of 7 human tumor models tested. ^[1]

Reference

[1] Judith S. Sebolt-Leopold et al. Proc Amer Assoc Cancer Res.2004,45