ADH-1 (Exherin) is a small, cyclic pentapeptide vascular-targeting agent with potential antineoplastic and antiangiogenic activities.
In vitro: Incubation with ADH-1 ata concentration of 0.2 mg/ml prevented collagen I-induced cell scattering. Incubating BxPC-3 cells with ADH-1 decreased cell motilityin response to collagen I.
In vivo: ADH-1 (Exherin) prevents N-cadherin overexpressing BxPC-3 cells tumor growth and metastasis in a mouse model for pancreatic cancer at 50 mg/kg (31 per day, 35 per week for 4 weeks) beginning 10days after surgical implantation of the tumor cells.
*The compound is unstable in solutions, freshly prepared is recommended
| Molecular Weight | 570.69 |
| Formula | C22H34N8O6S2 |
| CAS Number | 229971-81-7 |
| Solubility (25°C) | DMSO 45 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.
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