XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, exhibiting >50-fold selectivity over JAK1, JAK3 and TYK2.
 |
Source | Anticancer Res (2017). Figure 2. XL019 |
| Method | fluorescence-activated cell sorting analyses | |
| Cell Lines | KBV20C cancer cells | |
| Concentrations | 5 μM | |
| Incubation Time | 24 h | |
| Results | As shown in Figure 2A, co-treatment with XL019 and vincristine increased the number of cells arrested in the G2 phase compared to that observed with single treatments with either agent. |
| Molecular Weight | 444.53 |
| Formula | C25H28N6O2 |
| CAS Number | 945755-56-6 |
| 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.
[5] Constantine S Tam, et al. Investigational Janus kinase inhibitors
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