生物活性
BMS-754807是一种有效的，口服活性生长因子1受体/胰岛素受体家族靶向的激酶抑制剂。
Targets
| Target | Value |
| Insulin Receptor | IC50: 1.7nM |
| IGF-1R | IC50: 1.8nM |
| TrkB | IC50: 4.1nM |
| Met | IC50: 5.6nM |
| TrkA | IC50: 7.4nM |
| AuroraA | IC50: 9nM |
| AuroraB | IC50: 25nM |
| RON | IC50: 44nM |
| FLT3 | IC50: 170nM |
| JAK2 | IC50: 347nM |
| GSK-3β | IC50: 785nM |
| CDK2E | IC50: 795nM |
| MK2 | IC50: 919nM |
| LCK | IC50: 1.218μM |
| Src | IC50: 1.527μM |
| PKA | IC50: 1.605μM |
| PKCα | IC50: 2.53μM |
| BTK | IC50: 3.797μM |
| CSK | IC50: 5μM |
| PKCδ | IC50: 12μM |
| PKCζ | IC50: >50μM |
| PKCι | IC50: >50μM |
| p38α | IC50: >50μM |
| p38β | IC50: >50μM |
| HER1 | IC50: >50μM |
| IKK1 | IC50: >50μM |
| IKK2 | IC50: >50μM |
化学数据
| 目录号 | A11059 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 461.5 |
| Formula | C23H24FN9O |
| 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. | 1001350-96-4 |
| Synonyms | BMS754807, BMS 754807 |
| SMILES | C[C@]1(CCCN1C2=NN3C=CC=C3C(=N2)NC4=NNC(=C4)C5CC5)C(=O)NC6=CN=C(C=C6)F |
溶解度
| In vitro (25°C) | DMSO | 86 mg/mL (186.35 mM) |
| Water | Insoluble |
| Ethanol | 86 mg/mL |
| In vivo | 2% DMSO+30% PEG 300+ddH2O | 4 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 | 21.67 mL | 108.34 mL | 216.68 mL |
| 0.5 mM | 4.33 mL | 21.67 mL | 43.34 mL |
| 1 mM | 2.17 mL | 10.83 mL | 21.67 mL |
| 5 mM | 0.43 mL | 2.17 mL | 4.33 mL |
*The above data is based on the productmolecular weight 461.5 . 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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