生物活性
Dovitinib是一种小分子多靶点酪氨酸激酶抑制剂，可抑制通过ZNF198-FGFR1或BCR-FGFR1转化为IL3独立性的Ba / F3细胞，IC50值分别为150 nM和90 nM。
Targets
| Target | Value |
| FLT3 | IC50: 1nM |
| c-Kit | IC50: 2nM |
| FGFR1 | IC50: 8nM |
| VEGFR3/FLT4 | IC50: 8nM |
| FGFR3 | IC50: 9nM |
| VEGFR1/FLT1 | IC50: 10nM |
| VEGFR2/Flk1 | IC50: 13nM |
| PDGFRβ | IC50: 27nM |
| CSF-1R/c-Fms | IC50: 36nM |
| PDGFRα | IC50: 210nM |
| Insulin Receptor | IC50: 2μM |
| EGFR | IC50: 2μM |
| c-Met | IC50: >3μM |
| EphA2 | IC50: 4μM |
| Tie-2 | IC50: 4μM |
| IGF-1R | IC50: >10μM |
| HER2 | IC50: >10μM |
化学数据
| 目录号 | A10198 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 572.6 |
| Formula | C21H21FN6O.2C3H6O3 |
| 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. | 852433-84-2 |
| Synonyms | CHIR-258, TKI258 |
| SMILES | CC(C(=O)O)O.CC(C(=O)O)O.CN1CCN(CC1)C2=CC3=C(C=C2)N/C(=C/4\C(=C5C(=NC4=O)C=CC=C5F)N)/N3 |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 17.46 mL | 87.32 mL | 174.64 mL |
| 0.5 mM | 3.49 mL | 17.46 mL | 34.93 mL |
| 1 mM | 1.75 mL | 8.73 mL | 17.46 mL |
| 5 mM | 0.35 mL | 1.75 mL | 3.49 mL |
*The above data is based on the productmolecular weight 572.6. 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.
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