生物活性
EMD-1214063是MET酪氨酸激酶的抑制剂，IC50为4 nM，作用于c-Met比作用于IRAK4， TrkA， Axl， IRAK1和Mer选择性高200倍以上。具有潜在的抗肿瘤活性。它与MET酪氨酸激酶结合并破坏MET信号转导途径，这可能在过表达该激酶的肿瘤细胞中诱导凋亡。
Targets
| Target | Value |
| c-Met | IC50: 4nM |
| IRAK4 | IC50: 615nM |
| TrkA | IC50: 1.017μM |
| Axl | IC50: 1.566μM |
| IRAK1 | IC50: 2.037μM |
| Mer | IC50: 2.272μM |
| TrkB | IC50: 5.716μM |
| RON | IC50: >10μM |
化学数据
| 目录号 | A11257 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 492.6 |
| Formula | C29H28N6O2 |
| 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. | 1100598-32-0 |
| Synonyms | EMD1214063 |
| SMILES | CN1CCC(CC1)COC2=CN=C(N=C2)C3=CC(=CC=C3)CN4C(=O)C=CC(=N4)C5=CC=CC(=C5)C#N |
溶解度
| In vitro (25°C) | DMSO | Warmed: 4 mg/mL (8.12 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 5% DMSO+corn oil | 1 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 | 20.3 mL | 101.5 mL | 203 mL |
| 0.5 mM | 4.06 mL | 20.3 mL | 40.6 mL |
| 1 mM | 2.03 mL | 10.15 mL | 20.3 mL |
| 5 mM | 0.41 mL | 2.03 mL | 4.06 mL |
*The above data is based on the productmolecular weight 492.6 . 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.
