CNX-2006 is a novel irreversible epidermal growth factor receptor (EGFR) inhibitor. CNX-2006 exhibited specificity and potent in vitro and in vivo activity against T790M. In an in vitro resistance model, CNX-2006 significantly inhibited the emergence of resistant cells compared with erlotinib (1/24 vs 11/24, p = 0.0013). CNX-2006 selectively targets T790M, shows activity against other common and uncommon EGFR mutations, and does not select for resistance mediated by T790M. Additional studies are ongoing to elucidate mechanisms of acquired resistance to CNX-2006.
Molecular Weight | 545.53 |
Formula | C26H27F4N7O2 |
CAS Number | 1375465-09-0 |
Solubility (25°C) | DMSO |
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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