AZD8330

AZD8330 (ARRY-424704; ARRY-704) is a potent, selective, non-ATP competitive MEK1/2 inhibitor with IC50 of 7 nM; displays no inhibitory activity against a panel of >200 other kinases; demonstrates sub-nanomolar potency in mechanistic (pERK) and low to sub-nanomolar potency in functional (proliferation) assays in MEK1/2 inhibitor sensitive cell lines; inhibits ERK phosphorylation and causes tumor growth inhibition in Calu-6 rat xenograft.Solid Tumors Phase 1 Discontinued (In Vitro) :AZD8330 is a selective allosteric MEK1/ MEK2 inhibitor. Exposing human osteosarcoma cell lines MOS, U2OS, and 143B to a concentration of 0.5 μM of Trametinib, AZD8330 or TAK-733 for 6 hours, leads to loss of ERK phosphorylation indicating effective MEK inhibition.The activity of these three inhibitors is tested using concentration ranges in six osteosarcoma cell lines: MOS, U2OS, KPD, ZK58, 143b and Saos-2. All three inhibitors decrease viability of MOS and U2OS and strongly affect 143b. By contrast, viability of KPD, ZK58 and Saos-2 is not affected by any of the three inhibitors. (In Vivo) :In tumour xenograft models, AZD8330 demonstrates dose-dependent tumour growth inhibition of approximately 90% at tolerated doses (1.0 mg/kg once daily [OD]) .

869357-68-6

ARRY-424704 | ARRY-704 | AZD-8330 | ARRY424704 | ARRY704 | AZD8330

>98% (HPLC)

10 mM in DMSO

O=C (C (C=C1C) =C (NC2=CC=C (I) C=C2F) N (C) C1=O) NOCCO

C16H17FIN3O4

461.2267

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.