ARRY-380 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 100 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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