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PHA-739358 (Danusertib) is a small molecule with low nanomolar activity against all aurora kinases (AKs) with IC50 value of 13 nM for aurora-A and 79 nM for aurora-B respectively. PHA-739358 (Danusertib) also inhibits other cancer relevant tyrosine kinases such as wild type and mutated ABL, RET, TRK-A and FGFRs.
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Source | PLoS One (2014). Figure 1. PHA-739358 |
| Method | MTT assay | |
| Cell Lines | Ba/F3 cells | |
| Concentrations | 200 nM | |
| Incubation Time | 48 h | |
| Results | Accordingly, IC50 values were in a range of 150 nM for PHA-739358 and 10 nM for R763/AS703569, independent of the BCR-ABL mutation status |
| Cell Experiment | |
|---|---|
| Cell lines | wild-type (HCT-116 cells )or p53 −/− MEF (A2780) cells |
| Preparation method | Analysis of Cell Proliferation Analysis was done as previously described (20). Briefly, cells were seeded at different densities in 24-well plates with the appropriate medium. After 24 h, cells were treated with compound and incubated for 72 h at 37°C in 5% CO2 atmosphere. At the end of the incubation time, cells were detached from each plate and counted using a cell counter (Coulter Counter-Beckman). IC50 values were calculated using percent of growth versus untreated control. |
| Concentrations | 1μM |
| Incubation time | 24 or 48 hr |
| Animal Experiment | |
|---|---|
| Animal models | Mice bearing established A2780 and HCT-116 tumor xenografts |
| Formulation | saline |
| Dosages | 30 mg/kg bd for 5 consecutive days |
| Administration | i.v. |
| 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 | 474.55 |
| Formula | C26H30N6O3 |
| CAS Number | 827318-97-8 |
| Purity | >98% |
| Solubility | DMSO 50 mg/mL |
| Storage | at -20°C |
[3] Meulenbeld HJ, et al. Expert Opin Investig Drugs. Danusertib, an aurora kinase inhibitor.
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GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex. |
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