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
|Solubility (25°C)||DMSO 45 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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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