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MLN8054 is an orally bioavailable, highly selective small molecule inhibitor of Aurora with IC50s of 0.004uM and 0.172uM. for Aurora A and Aurora B.Auora kinase inhibitor MLN8054 binds to and inhibits Aurora kinase A, resulting in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregration, and inhibition of cell proliferation.
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Source | Int J Radiat Oncol Biol Phys (2011). Figure 1. MLN8054 |
| Method | Western blots | |
| Cell Lines | DU145 cells | |
| Concentrations | 1 μM | |
| Incubation Time | 1 h | |
| Results | When MLN8054 was administered in combination with radiation, total Aurora-A remained elevated, but phospho-Aurora-A levels were reduced nearly to baseline levels, indicating abrogation of Aurora-A activity |
| Cell Experiment | |
|---|---|
| Cell lines | HCT116, PC-3, SW480, DLD-1, MCF-7, MDA-MB-231, Calu-6, H460 and SKOV-3 cell lines |
| Preparation method | Cell Viability Analysis. Human tumor cell lines obtained from the American Type Culture Collection were grown in 96-well cell culture dishes according to the distributor's recommendations. MLN8054, diluted in DMSO, was added to the cells in 2-fold serial dilutions to achieve final concentrations ranging from 10 to 0.04 mM. MLN8054 at each dilution was added in triplicate with each replicate on a separate plate. Cells treated with DMSO (n = 6 wells per plate; 0.2% final concentration) served as the untreated control. The cells were treated with MLN8054 for 96 h at 37°C in a humidified cell culture chamber. Cell viability in each cell line was measured by using the Cell Proliferation ELISA, BrdU colorimetric kit according to the manufacturer's recommendations. |
| Concentrations | 0.04~10 mM |
| Incubation time | 96 hr |
| Animal Experiment | |
|---|---|
| Animal models | Female (HCT-116) and male (PC3) athymic nude NCR (nu/nu) mice |
| Formulation | 10% hydroxypropyl-β-cyclodextrin with 5% sodium bicarbonate |
| Dosages | 10 or 30 mg/kg BID or 30mg/kg QD for 21 consecutive days |
| Administration | orally |
| Molecular Weight | 476.86 |
| Formula | C25H15ClF2N4O2 |
| CAS Number | 869363-13-3 |
| Solubility (25°C) | DMSO 24 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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