生物活性
Cediranib (AZD2171)是一种高效的VEGFR(KDR)抑制剂，此外对c-Kit和PDGFRβ也具有相似的抑制活性，对VEGFR的选择性比PDGFR-α，CSF-1R和Flt3分别高36倍，110倍 和1000倍以上。
Targets
| Target | Value |
| VEGFR2/KDR | IC50: 0.5nM |
| c-Kit | IC50: 2nM |
| VEGFR3/FLT4 | IC50:<=3nM |
| VEGFR1/FLT1 | IC50: 5nM |
| PDGFRβ | IC50: 5nM |
| FGFR1 | IC50: 26nM |
| PDGFRα | IC50: 36nM |
| CSF-1R | IC50: 110nM |
| Src | IC50: 130nM |
| Abl | IC50: 260nM |
| FLT3 | IC50: >1μM |
| HER2/ErbB2 | IC50: >1μM |
| CDK2 | IC50: >1μM |
| CDK4 | IC50: >1μM |
| EGFR | IC50: 1.6μM |
| AuroraA | IC50: >10μM |
| AuroraB | IC50: >10μM |
| MEK | IC50: >10μM |
化学数据
| 目录号 | A10185 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 450.5 |
| Formula | C25H27FN4O3 |
| 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. | 288383-20-0 |
| Synonyms | Recentin |
| SMILES | CC1=CC2=C(N1)C=CC(=C2F)OC3=NC=NC4=CC(=C(C=C43)OC)OCCCN5CCCC5 |
溶解度
| In vitro (25°C) | DMSO | 80 mg/mL (177.57 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 5% DMSO+50% PEG 300+5% Tween+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 | 22.2 mL | 110.99 mL | 221.98 mL |
| 0.5 mM | 4.44 mL | 22.2 mL | 44.4 mL |
| 1 mM | 2.22 mL | 11.1 mL | 22.2 mL |
| 5 mM | 0.44 mL | 2.22 mL | 4.44 mL |
*The above data is based on the productmolecular weight 450.5 . 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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