Molecular Formula | C26H24N8O2 |
Molar Mass | 480.52 |
Density | 1.41±0.1 g/cm3(Predicted) |
pKa | 6.61±0.70(Predicted) |
Storage Condition | 2-8℃ |
In vitro study | ARRY-380 is a reversible, ATP-competitive inhibitor with a nanomolar inhibitory effect on ErbB2 in vitro and in cell assays. In cell experiments, ARRY-380 was 500-fold more selective for HER2 than for EGFR, and was as potent for truncated p95-HER2 as for HER2. |
In vivo study | ARRY-380 was able to inhibit tumor growth in a variety of her2-dependent tumor xenograft models. In many mouse tumor models, such as breast tumor (BT-474, MDA-MB-453), ovarian tumor (SKOV-3), gastric cancer (N87) model, have higher activity. In BT-474 models, ARRY-380 significantly inhibited tumor growth in a dose-dependent manner and mostly regressed. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.081 ml | 10.405 ml | 20.811 ml |
5 mM | 0.416 ml | 2.081 ml | 4.162 ml |
10 mM | 0.208 ml | 1.041 ml | 2.081 ml |
5 mM | 0.042 ml | 0.208 ml | 0.416 ml |