AZD8330 (C007B-020326)

InformationAZD8330 (ARRY704) is a novel, selective, non-ATP competitiveMEK 1/2inhibitor withIC50of 7 nM. Phase 1.In vitroAZD8330 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 vivoIn 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 Datacell lines：Concentrations：~10 μMIncubation Time：1 hourPowder Purity:≥99%. Specification: 10mM in DMSO Molecular Formula: C16H17FIN3O4 Molecular Weight: 461.23

UPC:

12352200

Condition:

New

Weight:

0.85 Ounces

HazmatClass:

No

Quantity:

1

Unit of Measurement:

EA

WeightUOM:

LB

MPN:

A409124-1ml

CAS:

869357-68-6

Product Size:

1ml