Vipivotide tetraxetan (PSMA-617) is a potent prostate-specific membrane antigen (PSMA) inhibitor with Ki value of 0.37 nM, it is used to make 177Lu-PSMA-617, which is a radioactive molecule to fight cancer. PSMA-617 has a high inhibition potency (equilibrium dissociation constant Ki=2.34±2.94 nM on LNCaP; Ki=0.37±0.21 nM enzymatically determined) and highly efficient internalization into LNCaP cells are demonstrated.
| Molecular Weight | 1042.14 |
| Formula | C49H71N9O16 |
| CAS Number | 1702967-37-0 |
| 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.
| Related PSMA Products |
|---|
| Glu-urea-Glu-NHS ester
Glu-urea-Glu-NHS ester is an active NHS Glu-urea-Glu that acts as a pharmacophore for binding to prostate-specific membrane antigen (PSMA) inhibitors. |
| PSMA-1007
PSMA-1007 is a prostate-specific membrane antigen (PSMA) ligand. |
| PSMA targeting peptide
PSMA-1 is a PSMA targeting peptide (GRFLTGGTGRLLRIS) and can be used for for targeted delivery of glucose-regulated protein (GRP)-silencing siRNAs in PCa cells. |
| Pelgifatamab
Pelgifatamab is a monoclonal antibody targeting prostate cancer-specific membrane antigen (PSMA) for prostate cancer-related studies. |
| ARX-517
ARX-517 is an antibody-coupled compound (ADC) targeting prostate-specific membrane antigen (PSMA), which can be used in prostate cancer-related studies. |
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