Product Data SheetProduct Name:CAS No.: Cat. No.:MWt:Formula:Purity :AZD8330869357-68-6HY-12058461.23C16H17FIN3O4>98%Solubility:DMSO ≥90mg/mL WaterDMSO90mg/mLWater<1.2mg/mL Ethanol ≥90mg/mLMechanisms: Pathways:MAPK ; Target:MEK Biological Activity:AZD8330(ARRY-424704; ARRY-704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitorAZD8330(ARRY424704ARRY704)illtiATPtitiMEK1/2ihibitwith IC50 of 7 nM. IC50 value: 7 nM [1] Target: MEK1/2 in vitro: AZD8330 potently and strongly inhibits MEK 1/2. AZD8330 has no inhibitory activity againstover 200 other kinases including at concentrations up to 10 μM. AZD8330 demonstrates sub-nanomolar potency in mechanistic (pERK) and low to sub-nanomolar potency in functional(proliferation) assays in MEK 1/2 inhibitor sensitive cell lines. invivo:InaCalu-6in vivo: In a Calu6 rat xenograft pharmacokinetic/pharmacodynamic (PK/PD) model a single, 1.25ratxenograftpharmacokinetic/pharmacodynamic(PK/PD)modelasingle125mg/kg oral dose of AZD8330 inhibits ERK phosphorylation by > 90% for between 4 and 8 hours.Doses as low as 0.4 mg/kg once daily are sufficient for > 80% tumor growth inhibition in the Calu-6nude rat xenograft model. In the Calu-6 model, AZD8330 inhibits tumor growth in a dose-dependentfas...References:[1]. Wallace EM, et al. AACR Annual Meeting, 2009, Abst 3696. Caution: Not fully tested. For research purposes onlyMedchemexpress LLCwww.medchemexpress.com18Wilkinson Way, Princeton, NJ 080,USAess.com Web: www.medchemexpress.comEmail: info@medchemexpr
