E3 ligase Ligand 4 (Thalidomide 4-fluoride) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein, it can connect to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1.
Molecular Weight | 276.22 |
Formula | C13H9FN2O4 |
CAS Number | 835616-60-9 |
Solubility (25°C) | DMSO ≥ 100 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.
[1] Mikołaj Słabicki, et al. Small-molecule-induced polymerization triggers degradation of BCL6
[3] Takumi Ito, et al. Molecular mechanisms of thalidomide and its derivatives
[4] Jun Araya, et al. PRKN-regulated mitophagy and cellular senescence during COPD pathogenesis
Related Ligand for E3 Ligase Products |
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2,6-bis(benzyloxy)-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine
2,6-bis(benzyloxy)-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine |
2,6-Bis(benzyloxy)pyridine-3-boronic acid
2,6-Bis(benzyloxy)pyridine-3-boronic acid |
2,6-Bis(benzyloxy)-3-bromopyridine
2,6-Bis(benzyloxy)-3-bromopyridine |
2,6-bis(benzyloxy)pyridin-3-amine
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3-[2,5-Difluoro-4-(4-piperidinyl)phenyl]-2,6-piperidinedione
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