VH032-cyclopropane-F is the VH032-based VHL ligand. VH032-cyclopropane-F can be connected to the ligand for protein (e.g., SMARCA BD ligand) by a linker to form PROTACs (e.g., PROTAC 1). PROTAC 1 is a partial degrader of SMARCA2 and SMARCA4.
| Molecular Weight | 532.63 |
| CAS Number | 2306193-99-5 |
| Solubility (25°C) | DMSO 90 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.
| Related Ligand for E3 Ligase Products |
|---|
| 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
2,6-bis(benzyloxy)pyridin-3-amine |
| 3-[2,5-Difluoro-4-(4-piperidinyl)phenyl]-2,6-piperidinedione
3-[2,5-Difluoro-4-(4-piperidinyl)phenyl]-2,6-piperidinedione |
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