VER-49009 is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β.
|Cell lines||Melanoma cells (SKMEL 2, SKMEL 5, SKMEL 28, WM266.4); Colon cancer cells (HCT116, BEneg, BE2, HT29, HT29oxaliR); Ovarian cancer cells (CH1, CH1doxR); Breast cancer cells (MB-231, MB-468, BT20, ZR751, MCF7, BT-474); nontumorigenic cells (HUVEC, MCF10a, PNT|
|Preparation method||Using the sulforhodamine B assay to mearsure antiproliferative effects . Determining HUVEC sensitivity by an alkaline phosphatase method.|
|Incubation time||4 days|
|Animal models||Mice bearing established OVCAR3 human ovarian xenografts|
|Formulation||10% DMSO, 5% Tween 20, 85% saline|
|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.
|Solubility||DMSO 60 mg/mL|
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