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GSK1070916 is a novel, highly potent and selective Aurora B/C kinases ATP competitive inhibitor with an EC50 of <10 nM. The protein kinases, Aurora A, B, and C have critical roles in the modulation of mitosis and are frequently overexpressed or amplified in human tumors. Human tumor cells treated with GSK1070916 revealed dose-dependent inhibition of phosphorylation on serine 10 of Histone H3, a substrate specific for Aurora B kinase. Moreover, GSK1070916 supprresses the proliferation of tumor cells. GSK1070916 displays dose-dependent inhibition of phosphorylation of an Aurora B–specific substrate in mice and consistent with its broad cellular activity, possesses antitumor effects in 10 human tumor xenograft models including breast, colon, lung, and two leukemia models. In another study, GSK1070916 selectively prevents AurB-INCENP (Ki=0.38 nM) and AurC-INCENP (Ki=1.5 nM) over AurA-TPX2 (target protein for Xenopus kinesin-like protein 2) (Ki=490 nM). Suppression of AurB-INCENP and AurC-INCENP is time-dependent, with an enzyme-inhibitor dissociation half-life of more than 480 min and 270 min respectively.
| Cell Experiment | |
|---|---|
| Cell lines | SW48, Colo 201, SW480, WiDr, Colo205, RKO E6, RKO, LoVo, HCT-116, SW620, HT29, W1417, DLD-1, HCT-8, Colo 320HSR, Hep-3B, OVCAR-3, MEC-1 cells |
| Preparation method | Plating cells in 96-well plates in the recommended growth media and incubated at 37 °C in 5% CO2 overnight. The following day, treating the cells with serial dilutions of GSK1070916. At this time, treating one set of cells with CellTiter-Glo for a time equal to 0 (T = 0) measurement. Following a 6- to 7-d incubation with compound, using the CellTiter-Glo reagent to measure cell proliferation according to the manufacture's recommended protocol. As inhibition of Aurora B induces endomitosis, the degree of which differs depending on the cell type, an extended compound treatment time is required to accurately reflect the effects on cell viability across a large panel of cell lines. For analysis of cell viability, values from wells with no cells are subtracted for background correction and the data plotted as a percent of the DMSO-treated control samples using Microsoft Excel XLfit4 software. The EC50 values represent the concentration of GSK1070916 where 50% maximal effect is observed |
| Concentrations | 0-15 mM |
| Incubation time | 6-7 days |
| Animal Experiment | |
|---|---|
| Animal models | Mice tumor xenograft models (A549, SW620, HCT116, H460, MCF-7, HL60, K562, Colo205) |
| Formulation | 2% Cremophor EL, 2% N,N-dimethylacetamide, and 96% acidified water (pH 5.0) |
| Dosages | 25, 50, or 100 mg/kg |
| Administration | Administered via i.p. once daily |
| Molecular Weight | 507.63 |
| Formula | C30H33N7O |
| CAS Number | 942918-07-2 |
| Solubility (25°C) | DMSO 100 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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