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PHA-680632 is the first representative of a new class of Aurora inhibitors (Aurora A/B/C IC50 at 27, 135 and 120 nM, respectively). This agent has a high potential for further development as an anticancer therapeutic. PHA-680632 is active on a wide range of cancer cell lines and shows significant tumor growth inhibition in different animal tumor models at well-tolerated doses. The IC50 of PHA-680632 for cell anti-proliferation ranged from 0.11 uM to 5.6 uM.
| Cell Experiment | |
|---|---|
| Cell lines | HeLa, HCT116, HT29, LOVO, DU145, and NHDF cells |
| Preparation method | Seeding cells (5 ×103 to 1.5 ×104 per cm2) in 24-well plate. 24 hours later, treating plates with PHA-680632 and incubating for 72 hours. At the end of incubation time, detaching cells from each plate and using a cell counter to count . Calculating IC50s using percentage of growth versus untreated cont |
| Concentrations | 0.001-1 μM, dissolved in DMSO as 10 mM stock solution |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | Mice (female athymic nude) xenografts models of p53−/− HCT116 cells |
| Formulation | Dissolved in 20% Tween-80 in 5% glucose solution |
| Dosages | 40 mg/kg |
| Administration | Intraperitoneal (i.p.) injection twice a day |
| Molecular Weight | 501.62 |
| Formula | C28H35N7O2 |
| CAS Number | 398493-79-3 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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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