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AT9283 is a potent inhibitor of several protein kinases, including Aurora A, Aurora B, Janus kinase 2 (JAK2), JAK3, and ABL. AT9283 potently inhibited proliferation and Jak2-related signalling in Jak2-dependent cell lines. The compound also demonstrated significant therapeutic potential in vivo in an ETV6-JAK2 (TEL-JAK2) murine leukaemia model.
| Cell Experiment | |
|---|---|
| Cell lines | HCT 116 cells |
| Preparation method | Primary HCT116 Cellular Assay. HCT 116 cells were cultured in DMEM + 10% FBS + GLUTAMAX I. Black 96-well flat bottomed (clear) tissue culture treated plates were seeded at 5 × 103 cells per well in 200 µL of medium and incubated for approximately 16 h at 37 °C in a humidified atmosphere of 5% CO2 in air. Cells were treated with test compound at nine different concentrations (spanning 1 nM to 10 µM, plus DMSO vehicle control) and then incubated for 72 h. Polyploidy morphological observations of the cells were then noted. The concentration of test compound required to produce a distinct polyploid phenotype was reported. |
| Concentrations | 1 nM to 10 µM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | HCT116 Colon Carcinoma Cell Line Xenograft Model |
| Formulation | 10% DMSO, 20% water, 70% hydroxypropyl--cyclodextrin (25% w/v aq) |
| Dosages | 15 and 20mg/kg twice daily (b.i.d. × 2, q4d) × 5 |
| Administration | intraperitoneal |
| Molecular Weight | 381.43 |
| Formula | C19H23N7O2 |
| CAS Number | 896466-04-9 |
| Solubility (25°C) | DMSO 61 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 |
|---|
| Phthalazinone pyrazole
Phthalazinone pyrazole is a potent, selective, and orally active inhibitor of Aurora-A kinase with an IC50 of 0.031 μM. |
| Aurora Kinases-IN-4
Aurora Kinases-IN-4 is a covalent and ATP competitive aurora kinase A inhibitor (IC50: 1.7 nM). |
| Derrone
Derrone, a prenylated isoflavones, is an Aurora kinase inhibitor, with IC50 values of 6 and 22.3 μM against Aurora B and Aurora A, respectively. Derrone shows anti-tumor activity. |
| CD532 hydrochloride
CD532 hydrochloride is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 hydrochloride has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 hydrochloride also can directly interact with AURKA and induces a global conformational shift. CD532 hydrochloride can be used for the research of cancer. |
| Aurora kinase inhibitor-2
Aurora kinase inhibitor-2 is a selective and ATP-competitive Aurora kinase inhibitor with IC50s of 310 nM and 240 nM for Aurora A and Aurora B, respectively. |
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