生物活性
PHA-680632是Aurora A，Aurora B和Aurora C的有效抑制剂，IC50分别为27 nM，135 nM和120 nM。对于FGFR1，FLT3，LCK，PLK1，STLK2和VEGFR2/3，它的IC50高10到200倍。
Targets
| Target | Value |
| AuroraA | IC50: 27nM |
| AuroraC | IC50: 120nM |
| AuroraB | IC50: 135nM |
| FGFR1 | IC50: 390nM |
| PLK1 | IC50: 780nM |
| FLT3 | IC50: 820nM |
| VEGFR3 | IC50: 1000nM |
| VEGFR2 | IC50: 1920nM |
| LCK | IC50: 1950nM |
| STLK2 | IC50: 5500nM |
化学数据
| 目录号 | A10714 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 501.6 |
| Formula | C28H35N7O2 |
| 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. | 398493-79-3 |
| Synonyms | PHA680632 |
| SMILES | CCC1=C(C(=CC=C1)CC)NC(=O)N2CC3=C(C2)NN=C3NC(=O)C4=CC=C(C=C4)N5CCN(CC5)C |
溶解度
| In vitro (25°C) | DMSO | 91 mg/mL (181.41 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 5% DMSO+50% PEG 300+5% Tween 80+ddH2O | 14 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 | 19.94 mL | 99.68 mL | 199.36 mL |
| 0.5 mM | 3.99 mL | 19.94 mL | 39.87 mL |
| 1 mM | 1.99 mL | 9.97 mL | 19.94 mL |
| 5 mM | 0.4 mL | 1.99 mL | 3.99 mL |
*The above data is based on the productmolecular weight 501.6 . 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.
