AZD8330 (ARRY704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.
Storage Temp
Store at -80°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
Product Description
Information
AZD8330 (ARRY704) is a novel, selective, non-ATP competitiveMEK 1/2inhibitor withIC50of 7 nM. Phase 1. In vitro
AZD8330 potently and strongly inhibits MEK 1/2. AZD8330 has no inhibitory activity against over 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.
In vivo
In a Calu-6 rat xenograft pharmacokinetic/pharmacodynamic (PK/PD) model a single, 1.25 mg/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-6 nude rat xenograft model. In the Calu-6 model, AZD8330 inhibits tumor growth in a dose-dependent fashion, at 0.3 mg/kg and 1.0 mg/kg once daily. Cell Data
cell lines：
Concentrations：~10 μM
Incubation Time：1 hour
Powder Purity:≥99%
Product Properties
ALogP
1.653
hba_count
3
HBD Count
3
Rotatable Bond
6
Associated Targets(Human)
MAP2K2TclinDual specificity mitogen-activated protein kinase kinase 2 (1 Activities)
