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.