PD0325901 is non-competitive with ATP and is exquisitely specific and highly potent against purified MEK, exhibiting a Kiapp 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

June 21, 2017

prudect name : PD0325901 is non-competitive with ATP and is exquisitely specific and highly potent against purified MEK, exhibiting a Kiapp 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
PD 0325901

Synonyms: CAS NO: 391210-10-9Molecular Formula: C16H14F3IN2O4Molecular Weight: 482.19Purity: 98% minSolubility: In DMSOStorage: −20°C


web site: www.medchemexpress.com

References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18538737