生物活性
Tivozanib (AV-951)是一种口服VEGF受体酪氨酸激酶抑制剂，旨在抑制所有三种VEGF受体。
Targets
| Target | Value |
| VEGFR2 | IC50: 6.5nM |
| VEGFR3 | IC50: 15nM |
| EphB2 | IC50: 24nM |
| VEGFR1 | IC50: 30nM |
| PDGFRα | IC50: 40nM |
| PDGFRβ | IC50: 49nM |
| c-Kit | IC50: 78nM |
| Tie-2 | IC50: 78nM |
| EphB4 | IC50: 480nM |
| FGFR1 | IC50: 530nM |
| c-Met | IC50: 550nM |
| Abl | IC50: 620nM |
| Src | IC50: 960nM |
| FGFR3 | IC50: >1μM |
| FGFR4 | IC50: >1μM |
| FLT3 | IC50: >1μM |
| EGFR | IC50: >1μM |
| ErbB2 | IC50: >1μM |
| Insulin Receptor | IC50: >1μM |
| FAK | IC50: >1μM |
| ErbB4 | IC50: >1μM |
| IGF-1R | IC50: >1μM |
| JAK2 | IC50: >1μM |
化学数据
| 目录号 | A10101 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 454.9 |
| Formula | C22H19ClN4O5 |
| 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. | 475108-18-0 |
| Synonyms | AV-951, AV951 |
| SMILES | CC1=CC(=NO1)NC(=O)NC2=C(C=C(C=C2)OC3=C4C=C(C(=CC4=NC=C3)OC)OC)Cl |
溶解度
| In vitro (25°C) | DMSO | 19 mg/mL (41.76 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 2% DMSO+30% PEG 300+ddH2O | 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 | 21.98 mL | 109.91 mL | 219.83 mL |
| 0.5 mM | 4.4 mL | 21.98 mL | 43.97 mL |
| 1 mM | 2.2 mL | 10.99 mL | 21.98 mL |
| 5 mM | 0.44 mL | 2.2 mL | 4.4 mL |
*The above data is based on the productmolecular weight 454.9 . 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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