AZD3463 is a novel inhibitor of ALK which overcomes multiple mechanisms of acquired resistance to crizotinib. AZD3463 inhibits ALK with a Ki value of 0.75 nM. AZD3463 dose-dependently inhibits pALK in tumor xenografts in vivo, resulting in stasis (H3122) or regression (DEL, H2228) in tumor volume. AZD3463 obtains equivalent potency to mutantL1196M and wild-type ALK in vivo.
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Source | Sci Rep (2016). Figure 2. AZD3463 |
| Method | colony formation assay | |
| Cell Lines | NB cells | |
| Concentrations | 5 μM | |
| Incubation Time | 4 hrs | |
| Results | Our data indicates that AZD3463 effectively blocks both anchorage-dependent and independent colony formation of NB cells. |
| Molecular Weight | 448.95 |
| Formula | C24H25ClN6O |
| CAS Number | 1356962-20-3 |
| Solubility (25°C) | DMSO 20 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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