生物活性
AZD1152-HQPA (Barasertib)是Aurora B的高效抑制剂，Ki值分别为0.36（Aurora B）和1369 nM（Aurora A），与一组其他50种激酶相比具有很高的特异性。
靶点信息
| Aurora B (Cell-free assay) | Aurora A (Cell-free assay) | | | |
| 0.37 nM | 1368 nM | | | |
化学数据
| 目录号 | A10109 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 507.7 |
| Formula | C26H30FN7O3 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 722544-51-6 |
| Synonyms | Barasertib |
| SMILES | CCN(CCCOC1=CC2=C(C=C1)C(=NC=N2)NC3=NNC(=C3)CC(=O)NC4=CC(=CC=C4)F)CCO |
溶解度
| In vitro (25°C) | DMSO | 93 mg/mL (183.23 mM) |
| Water | Insoluble |
| Ethanol | 3 mg/mL (5.91 mM) |
| In vivo | 2% DMSO+40% PEG 300+2% Tween 80+ddH2O | 6 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. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 19.7 mL | 98.48 mL | 196.97 mL |
| 0.5 mM | 3.94 mL | 19.7 mL | 39.39 mL |
| 1 mM | 1.97 mL | 9.85 mL | 19.7 mL |
| 5 mM | 0.39 mL | 1.97 mL | 3.94 mL |
*The above data is based on the productmolecular weight 507.7 . 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.
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