PROTAC BTK degraders-5is a selective BTK degrader with a DC50 value of 7.0 nM in JeKo-1 cells.
| Molecular Weight | 958.52 |
| Formula | C52H57ClFN9O6 |
| 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.
[1] Daniel Schaefer et al. Pharmaceuticals (Basel). Recent Advances in Covalent Drug Discovery
[3] Zi Liu et al. Mol Biomed. An overview of PROTACs: a promising drug discovery paradigm
[4] Tingting Yao et al. Int J Mol Sci. Recent Advances in PROTACs for Drug Targeted Protein Research
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| NX-2127
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