生物活性
NVP-BHG712是EphB4激酶的选择性抑制剂，在体外对EphB4的选择性超过40多种其他激酶（包括FGFR3）。
Targets
| Target | Value |
| EphB4 | ED50 | 25nM |
| C-Raf | IC50: 0.395μM |
| c-Src | IC50: 1.266μM |
| c-Abl | IC50: 1.667μM |
| Tie-2 | IC50: >10μM |
| Axl | IC50: >10μM |
| HER1 | IC50: >10μM |
| PKA | IC50: >10μM |
| CDK1 | IC50: >10μM |
| PKB | IC50: >10μM |
| PDK-1 | IC50: >10μM |
| FGFR3 | IC50: >10μM |
| c-Met | IC50: >10μM |
化学数据
| 目录号 | A10661 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 503.5 |
| Formula | C26H20F3N7O |
| 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. | 940310-85-0 |
| Synonyms | NVPBHG712 |
| SMILES | CC1=C(C=C(C=C1)C(=O)NC2=CC=CC(=C2)C(F)(F)F)NC3=NC(=NC4=C3C=NN4C)C5=CN=CC=C5 |
溶解度
| In vitro (25°C) | DMSO | 90 mg/mL (178.75 mM) |
| Water | Insoluble |
| Ethanol | 3 mg/mL (5.95 mM) |
| In vivo | NMP+PEG300 (10+90, v+v) | 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 | 19.86 mL | 99.3 mL | 198.61 mL |
| 0.5 mM | 3.97 mL | 19.86 mL | 39.72 mL |
| 1 mM | 1.99 mL | 9.93 mL | 19.86 mL |
| 5 mM | 0.4 mL | 1.99 mL | 3.97 mL |
*The above data is based on the productmolecular weight 503.5 . 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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