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Tozasertib (VX-680, MK-0457) is a small-molecule Aurora kinase inhibitor. The Aurora kinases are essential for the regulation of chromosome segregation and cytokinesis during mitosis. Tozasertib (VX-680) blocks cell-cycle progression and induces apoptosis in a diverse range of human tumor types. Tozasertib (VX-680) effectively inhibits proliferation of several different cell lines of clear cell renal carcinoma (IC50s < 10 μM) and blocks the growth of tumors in a rodent model of cancer (80 mg/kg), inhibiting H3 histone phosphorylation, to an increase of apoptotic cells, and to morphological changes such as vacuolization and swelling of the cells and nuclei. The combination of VX-680 and histone deacetylase inhibitor SAHA had a synergistic effect on the proliferation of HUH6 cells. Tozasertib (VX-680) might improve treatment results in HB with increased Aurora kinase activity by inhibiting cell proliferation and induction of apoptosis.
Pharmaceuticals (Basel). 2024 Sep 21;17(9):1245.
Molecular Targets of Minor Cannabinoids in Breast Cancer: In Silico and In Vitro Studies
Tozasertib purchased from AbMole
J Hematol Oncol. 2017 Jun 8;10(1):115.
SIX3, a tumor suppressor, inhibits astrocytoma tumorigenesis by transcriptional repression of AURKA/B
Tozasertib purchased from AbMole
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Source | Journal of Hematology & Oncology (2017). Figure 7. VX680 (Abmole Bioscience) |
| Method | CCK8 assay | |
| Cell Lines | U251, U87 and U118 cell lines | |
| Concentrations | ||
| Incubation Time | 48 and 72 h | |
| Results | We found that the U251-SIX3 cells showed less sensitivity to VX680 compared with the U251-CON cells (Fig. 7a). With increased expression of AURKA or AURKB and reduced expression of SIX3, the p53 mutant U251 cells were more sensitive to VX680 treatment, compared with the p53 wild-type U87 cells (Fig. 7b). |
| Cell Experiment | |
|---|---|
| Cell lines | SW620, K562, HL-60, MIA PaCa-2 and HCT116 cells |
| Preparation method | Analysis of cell proliferation and viability. Tumor cells were seeded in 96-well plates and incubated with VX-680 for 96 h. To measure DNA synthesis, 0.5 mCi of [3H]thymidine was added to each well 3 h before the end of the experiment. Cells were then collected, and the incorporated radioactivity was counted on a Wallac microplate beta-counter. Cell viability was assessed using Promega CellTiter 96AQ to measure MTS (3-(4,5 dimethylthiazol-2-yl)-5-(3- carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt) conversion. |
| Concentrations | 1~10 μM |
| Incubation time | 96 h |
| Animal Experiment | |
|---|---|
| Animal models | female athymic NCr-nu mice HL-60, MIA PaCa-2 and HCT116 cells tumour xenograft model |
| Formulation | 50% PEG 300 in 50 mM phosphate buffer |
| Dosages | q.4.d. at a dose of 12.5, 25, 50 and 75 mg/kg |
| Administration | i.v. |
| Molecular Weight | 464.59 |
| Formula | C23H28N8OS |
| CAS Number | 639089-54-6 |
| Solubility (25°C) | DMSO 75 mg/mL |
| Storage | 2-8°C, protect from light, dry, sealed |
| 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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