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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. |
| Molecular Weight | 474.55 |
| Formula | C26H30N6O3 |
| CAS Number | 827318-97-8 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Meulenbeld HJ, et al. Expert Opin Investig Drugs. Danusertib, an aurora kinase inhibitor.
| Related Aurora Kinase Products |
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AZD1152-HQPA (Barasertib) is a highly potent and selective inhibitor of Aurora with Ki values of 0.36 and 1369 nM for Aurora B and Aurora A respectively. |
| CCT-129202
CCT129202 is an Aurora kinase inhibitor with IC50 of 0.042 ± 0.022, 0.198 ± 0.05, and 0.227 ± 0.064 μmol/L for Aurora A, Aurora B, and Aurora C, respectively. |
| CYC116
CYC116 is a potent, small molecule inhibitor of Aurora A, B and C with IC50 value of 44, 19 and 65 nM respectively. CYC-116 also inhibits VEGFR2, Src, Lck AND FLT3 with with Kis of 44, 82, 280, 44 nM, respectively. CYC-116 may have broad-spectrum antitumor activity. |
| ENMD-2076
ENMD-2076 is an orally-active, Aurora A/angiogenic kinase inhibitor. |
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