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 | A11411 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 392.4 |
| Formula | C21H21FN6O |
| 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. | 405169-16-6 |
| Synonyms | CHIR-258, CHIR258, TKI258 |
| SMILES | CN1CCN(CC1)C2=CC3=C(C=C2)N/C(=C\4/C(=C5C(=NC4=O)C=CC=C5F)N)/N3 |
溶解度
| In vitro (25°C) | DMSO | 28 mg/mL (71.34 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 30% PEG400+0.5% Tween80+5% propylene glycol | 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 | 25.48 mL | 127.42 mL | 254.84 mL |
| 0.5 mM | 5.1 mL | 25.48 mL | 50.97 mL |
| 1 mM | 2.55 mL | 12.74 mL | 25.48 mL |
| 5 mM | 0.51 mL | 2.55 mL | 5.1 mL |
*The above data is based on the productmolecular weight 392.4 . 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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