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TAK-901 is an investigational, multitargeted Aurora B kinase inhibitor with potential antineoplastic activity. TAK-901 potently inhibited only a few kinases other than Aurora B in intact cells, including FLT3 and FGFR2. TAK-901 inhibited cell proliferation with effective concentration values from 40 to 500 nmol/L in various human cancer cell lines. TAK-901 suppressed cellular histone H3 phosphorylation and induced polyploidy. TAK-901 displayed potent activity against several leukemia models. In rodent xenografts, TAK-901 exhibited potent activity against multiple human solid tumor types, and complete regression was observed in the ovarian cancer A2780 model. In vivo studies showed that TAK-901 induced pharmacodynamic responses consistent with Aurora B inhibition and correlating with retention of TAK-901 in tumor tissue. TAK-901 is currently in a phase I clinical trials in patients within a diverse range of cancers.
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Source | Anticancer Res (2017). Figure 1. TAK-901 |
| Method | FACS analysis | |
| Cell Lines | HCT116 cells | |
| Concentrations | 100 nM | |
| Incubation Time | 72 h | |
| Results | Induction of polyploidy was also detected by FACS analysis; 2N and 4N cells were observed in DMSO-treated HCT116 cells, while mainly 4N and 8N were observed in TAK-901- or AZD1152-HQPA-treated HCT116 cells |
| Cell Experiment | |
|---|---|
| Cell lines | A2780, A375, A549, COLO-205, HCT116, PC-3 cells line |
| Preparation method | Cell proliferation and viability assays. Cells were plated in 96-well microtiter plates and incubated with serial dilutions of TAK-901 for 72 hours. Cell proliferation was determined by ELISA analysis of bromodeoxyuridine (BrdUrd) incorporation into DNA. IMR-90 immortalized lung fibroblasts were seeded in 96-well microtiter plates and cultured for 3 to 4 days until confluent. Cells were then incubated with serial dilutions of TAK-901 for 72 hours. The MTS assay was conducted as per the manufacturer's instructions. The concentration of TAK-901 required to inhibit half of the maximal effective concentration (EC50) was determined from the dose–response curves. |
| Concentrations | 0~8 μM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | Nude mice or rats Xenograft models |
| Formulation | 12% Captisol, 25 mmol/L citrate, pH 3.0 |
| Dosages | 5 μL/mg twice daily |
| Administration | intravenously |
| Molecular Weight | 504.64 |
| Formula | C28H32N4O3S |
| CAS Number | 934541-31-8 |
| Solubility (25°C) | DMSO 10 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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