生物活性
R547是一种新型的细胞周期和转录周期依赖性激酶（CDKs）选择性抑制剂（CDK1，CDK2和CDK4分别为Ki = 1、3和1 nM），具有出色的体外细胞效价，可抑制各种细胞的生长。人肿瘤细胞系。
Targets
| Target | Value |
| CDK4/CyclinD1 | ki: 1nM |
| CDK1/CyclinB | ki: 2nM |
| CDK2/CyclinE | ki: 3nM |
| PKA | ki: >5μM |
| PKB | ki: >5μM |
| PKCα | ki: >5μM |
| PKCβ | ki: >5μM |
| Fyn | ki: >5μM |
| EphB3 | ki: >5μM |
| SGK | ki: >5μM |
| KDR | ki: >5μM |
| FGFR | ki: >5μM |
| EGFR | ki: >5μM |
| PDGFR | ki: >5μM |
| IGFR | ki: >5μM |
| Src | ki: >5μM |
| FAK | ki: >5μM |
| AuroraA | ki: >5μM |
| GSK-3β | ki: 8μM |
| p38 | ki: >50μM |
| MAPK2 | ki: >50μM |
化学数据
| 目录号 | A11190 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 441.45 |
| Formula | C18H21F2N5O4S |
| 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. | 741713-40-6 |
| Synonyms | R-547 |
| SMILES | COC1=C(C(=C(C=C1)F)F)C(=O)C2=CN=C(N=C2N)NC3CCN(CC3)S(=O)(=O)C |
溶解度
| In vitro (25°C) | DMSO | 56 mg/mL (126.85 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 1% hydroxyethyl cellulose+0.2% Tween 80 | 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 | 22.65 mL | 113.26 mL | 226.53 mL |
| 0.5 mM | 4.53 mL | 22.65 mL | 45.31 mL |
| 1 mM | 2.27 mL | 11.33 mL | 22.65 mL |
| 5 mM | 0.45 mL | 2.27 mL | 4.53 mL |
*The above data is based on the productmolecular weight 441.45. 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.
