生物活性
BX-912是3-磷酸肌醇依赖性激酶1（PDK1）的抑制剂。
Targets
| Target | Value |
| PDK-1 | IC50: 12nM |
| PKA | IC50: 110nM |
| KDR | IC50: 410nM |
| CDK2/CyclinE | IC50: 650nM |
| Chk1 | IC50: 830nM |
| c-Kit | IC50: 850nM |
| PKC | IC50: 1.25μM |
| T-Fyn | IC50: 2.1μM |
| Insulin Receptor | IC50: 6.1μM |
| GSK-3β | IC50: 7.4μM |
| EGFR | IC50: >10μM |
化学数据
| 目录号 | A11149 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 471.4 |
| Formula | C20H23BrN8O |
| 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. | 702674-56-4 |
| Synonyms | BX912 |
| SMILES | C1CCN(C1)C(=O)NC2=CC=CC(=C2)NC3=NC=C(C(=N3)NCCC4=CN=CN4)Br |
溶解度
| In vitro (25°C) | DMSO | 80 mg/mL (169.72 mM) |
| Water | Insoluble |
| Ethanol | 80 mg/mL (169.72 mM) |
| In vivo | 30% PEG400+0.5% Tween80+5% propylene glycol | 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 | 21.21 mL | 106.07 mL | 212.13 mL |
| 0.5 mM | 4.24 mL | 21.21 mL | 42.43 mL |
| 1 mM | 2.12 mL | 10.61 mL | 21.21 mL |
| 5 mM | 0.42 mL | 2.12 mL | 4.24 mL |
*The above data is based on the productmolecular weight 471.4 . 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.
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