TuCATinib 是可口服的选择性HER2抑制剂，IC50为8 nM。

Irbinitinib(ARRY-380; ONT-380) is a potent and selective HER2 inhibitor (IC50: 8 nM).

Irbinitinib selectively binds to and inhibits the phosphorylation of ErbB-2, which may prevent the activation of ErbB-2 signal transduction pathways, resulting in growth inhibition and death of ErbB-2-expressing tumor cells.

In vivo, ARRY-380 significantly inhibits tumor growth in multiple HER2-dependent tumor xenograft models[2]. It shows excellent activity in numerous mouse tumor models including breast (BT-474, MDA-MB-453), ovarian (SKOV-3) and gastric (N87) carcinoma models. In the BT-474 model, ARRY-380 demonstrated significant dose-related tumor growth inhibition (TGI; 50% at 50 mg/kg/d and 96% at 100 mg/kg/d) with numerous partial regressions (>50% reduction from baseline size)[1].

937263-43-9

C26H24N8O2

480.52

ARRY-380;ONT-380;Irbinitinib

Ethanol:15 mg/mL (31.22 mM)
DMSO:87 mg/mL(181.1 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years