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ARRY-380 analog is an orally bioavailable, potent, selective, small-molecule tyrosine kinase HER2 and p95-HER2 inhibitor with an IC50 of 8 and 7 nM, respectively. However, ARRY-380 inhibits EGFR with an IC50 of 4 μM. ARRY-380 is about 500-fold selective for HER2 versus EGFR. ARRY-380 produces significantly antitumor activities in multiple HER2-dependent tumor xenograft models and generates additive activity in combination with standard-of-care agents. ARRY-380 is in a phase I clinical trial for the treatment of breast cancer
| Molecular Weight | 569.63 |
| Formula | C29H27N7O4S |
| CAS Number | 937265-83-3 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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