VHL Ligand 1 hydrochloride is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. VHL Ligand 1 is potential useful for the targeted degradation of the androgen receptor. VHL ligand 1 hydrochloride can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.
| Molecular Weight | 467.02 |
| Formula | C22H31ClN4O3S |
| CAS Number | 1448189-80-7 |
| Solubility (25°C) | Water ≥ 50 mg/mL DMSO ≥ 30 mg/mL |
| Storage | -20°C, dry, sealed, protect from light |
| 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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