AZD8330

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AZD8330 (ARRY-424704;ARRY-704) 是一种有效的、选择性的、非 ATP 竞争性 MEK1/2 抑制剂，IC50 为 7 nM。

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]).

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 tumour xenograft models, AZD8330 demonstrates dose-dependent tumour growth inhibition of approximately 90% at tolerated doses (1.0 mg/kg once daily [OD]).

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

MAPK/ERK Signaling

MEK

ERKphosphorylation|MEK1/2

Cancer

Solid Tumors

869357-68-6

461.2267

C16H17FIN3O4

>98% (HPLC)

10 mM in DMSO

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

3-Pyridinecarboxamide, 2-[(2-fluoro-4-iodophenyl)amino]-1,6-dihydro-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-

(-20℃)

With Ice Pack

≥ 2 years