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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 |
|---|
| 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. |
| MLN8054
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. |
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