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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 |
|---|
| AT9283
AT9283 is a potent inhibitor of several protein kinases, including Aurora A, Aurora B, Janus kinase 2 (JAK2), JAK3, and ABL. |
| AZD1152-HQPA
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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