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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 |
|---|
| Phthalazinone pyrazole
Phthalazinone pyrazole is a potent, selective, and orally active inhibitor of Aurora-A kinase with an IC50 of 0.031 μM. |
| Aurora Kinases-IN-4
Aurora Kinases-IN-4 is a covalent and ATP competitive aurora kinase A inhibitor (IC50: 1.7 nM). |
| Derrone
Derrone, a prenylated isoflavones, is an Aurora kinase inhibitor, with IC50 values of 6 and 22.3 μM against Aurora B and Aurora A, respectively. Derrone shows anti-tumor activity. |
| CD532 hydrochloride
CD532 hydrochloride is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 hydrochloride has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 hydrochloride also can directly interact with AURKA and induces a global conformational shift. CD532 hydrochloride can be used for the research of cancer. |
| Aurora kinase inhibitor-2
Aurora kinase inhibitor-2 is a selective and ATP-competitive Aurora kinase inhibitor with IC50s of 310 nM and 240 nM for Aurora A and Aurora B, respectively. |
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