生物活性
MLN8054是一种有效的，选择性Aurora A抑制剂，在Sf9昆虫细胞中IC50为4 nM，作用于Aurora A比作用于Aurora B选择性高40倍，可在体内和体外诱导人肿瘤细胞衰老。
Targets
| Target | Value |
| AuroraA | IC50: 4nM |
| AuroraB | IC50: 172nM |
| LCK | IC50: 3.2μM |
| PKA | IC50: 19μM |
| CK2 | IC50: 20.5μM |
| Chk2 | IC50: 28μM |
| PLK1 | IC50: 53μM |
| Chk1 | IC50: >100μM |
| PKC | IC50: >100μM |
| CaMKII | IC50: >100μM |
| CDK2E | IC50: >100μM |
| CDK1 | IC50: >100μM |
化学数据
| 目录号 | A10601 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 476.9 |
| Formula | C25H15ClF2N4O2 |
| 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. | 869363-13-3 |
| Synonyms | MLN-8054 |
| SMILES | C1C2=CN=C(N=C2C3=C(C=C(C=C3)Cl)C(=N1)C4=C(C=CC=C4F)F)NC5=CC=C(C=C5)C(=O)O |
溶解度
| In vitro (25°C) | DMSO | 91 mg/mL (190.82 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 15% Captisol | 28 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 | 20.97 mL | 104.84 mL | 209.69 mL |
| 0.5 mM | 4.19 mL | 20.97 mL | 41.94 mL |
| 1 mM | 2.1 mL | 10.48 mL | 20.97 mL |
| 5 mM | 0.42 mL | 2.1 mL | 4.19 mL |
*The above data is based on the productmolecular weight 476.9 . 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.
m.cnreagent.com