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VER-49009 is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β.
| Cell Experiment | |
|---|---|
| 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. |
| Concentrations | ~10 μM |
| Incubation time | 4 days |
| Animal Experiment | |
|---|---|
| Animal models | Mice bearing established OVCAR3 human ovarian xenografts |
| Formulation | 10% DMSO, 5% Tween 20, 85% saline |
| Dosages | ~4 mg/kg |
| Administration | i.p. |
| 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.
| Molecular Weight | 387.82 |
| Formula | C19H18ClN3O4 |
| CAS Number | 940289-57-6 |
| Purity | >98% |
| Solubility | DMSO 60 mg/mL |
| Storage | at -20°C |
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