17-DMAG hydrochloride (Alvespimycin), a watersoluble geldanamycin analog belonging to the class of benzoquinones, is a selective Hsp90 inhibitor. 17-DMAG hydrochloride binds to the N-terminal domain ATP binding site of Hsp90, inhibiting Hsp90 chaperone activity. 17-DMAG hydrochloride demonstrates greater potency and water solubility than other geldanamycin analogs such as 17-AAG (mean GI50 values are 53 and 123 nM for 17-DMAG hydrochloride and 17-AAG respectively), while demonstrating anti-tumor activity and offering excellent oral bioavailability.
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 100 mg/mL|
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