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- Tomoya Takeda, .et al. AT9283 exhibits antiproliferative effect on tyrosine kinase inhibitor-sensitive and -resistant chronic myeloid leukemia cells by inhibition of Aurora A and Aurora B, Oncol Rep, 2020, August 18
Biological Activity
AT9283 inhibits aurora kinase A and B and targets other tyrosine and serine/threonine kinases associated with myeloid cell proliferation.
Targets
| Target | Value |
|---|---|
| JAK3 | IC50: 1.1nM |
| JAK2 | IC50: 1.2nM |
| AuroraA | IC50: ~3.0nM |
| AuroraB | IC50: ~3.0nM |
| Abl1(T315I) | IC50: 4nM |
| GSK-3β | IC50: 1nM-10nM |
| FGFR2 | IC50: 1-10nM |
| VEGFR3/FLT4 | IC50: 1nM-10nM |
| Mer | IC50: 1nM-10nM |
| RET | IC50: 1nM-10nM |
| RSK2 | IC50: 1nM-10nM |
| RSK3 | IC50: 1nM-10nM |
| TYK2 | IC50: 1nM-10nM |
| YES | IC50: 1nM-10nM |
| Abl(Q252H) | IC50: 10nM-30nM |
| DRAK1 | IC50: 10nM-30nM |
| FGFR1 | IC50: 10nM-30nM |
| FGFR1(V561M) | IC50: 10nM-30nM |
| FGFR2(N549H) | IC50: 10nM-30nM |
| FGFR3 | IC50: 10nM-30nM |
| VEGFR1/FLT1 | IC50: 10nM-30nM |
| FLT3 | IC50: 10nM-30nM |
| PDGFRα(D842V) | IC50: 10nM-30nM |
| PDK-1 | IC50: 10nM-30nM |
| PKCμ | IC50: 10nM-30nM |
| RSK4 | IC50: 10nM-30nM |
| Src(T341M) | IC50: 10nM-30nM |
| VEGFR2 | IC50: 10nM-30nM |
| In vitro (25°C) | DMSO | 68 mg/mL (178.28 mM) | |
| Water | Insoluble | ||
| Ethanol | 34 mg/mL (89.13 mM) | ||
| In vivo | 2% DMSO+30% PEG 300+ddH2O | 4 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 26.22 mL | 131.1 mL | 262.19 mL |
| 0.5 mM | 5.24 mL | 26.22 mL | 52.44 mL |
| 1 mM | 2.62 mL | 13.11 mL | 26.22 mL |
| 5 mM | 0.52 mL | 2.62 mL | 5.24 mL |
*The above data is based on the productmolecular weight 381.4. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A10095 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 896466-04-9 |
| Formula | C19H23N7O2 |
| M. Wt | 381.4 |
| Purity | >98% |
| SMILES | C1CC1NC(=O)NC\2=CNN/C2=C\3/N=C4C=CC(=CC4=N3)CN5CCOCC5 |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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