PD173955 is a potent Bcr-Abl inhibitor with IC50 of 1-2 nM, also inhibiting Src activity with IC50 of 22 nM.
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Source | Vascul Pharmacol (2013). Figure 1. PD173955 |
| Method | western blot | |
| Cell Lines | HAECs | |
| Concentrations | 5 μM | |
| Incubation Time | 30 min | |
| Results | PD173955 and PP2 suppressed PLC-induced increase in eNOS phosphorylation and activity. |
| Molecular Weight | 443.35 |
| Formula | C21H16Cl2N4OS |
| CAS Number | 260415-63-2 |
| Solubility (25°C) | DMSO 15 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.
[3] George A Kraus, et al. New effective inhibitors of the Abelson kinase
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