生物活性
Axitinib是一种小分子酪氨酸激酶抑制剂，可抑制多种靶标，包括VEGFR-1，VEGFR-2，VEGFR-3，血小板衍生生长因子受体（PDGFR）和cKIT（CD117）。
Targets
| Target | Value |
| VEGFR1/FLT1 | IC50: 0.1nM |
| VEGFR2/Flk1 | IC50: 0.18nM |
| VEGFR2/KDR | IC50: 0.2nM |
| VEGFR3 | IC50: 0.1nM-0.3nM |
| PDGFRβ | IC50: 1.6nM |
| Kit | IC50: 1.7nM |
| PDGFRα | IC50: 5.0nM |
| CSF-1R | IC50: 73nM |
| FLT3 | IC50: >1μM |
化学数据
| 目录号 | A10103 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 386.5 |
| Formula | C22H18N4OS |
| 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. | 319460-85-0 |
| Synonyms | AG 013736 |
| SMILES | CNC(=O)C1=CC=CC=C1SC2=CC3=C(C=C2)C(=NN3)/C=C/C4=CC=CC=N4 |
溶解度
| In vitro | DMSO | Warmed: 30 mg/mL (77.62 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
*<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 | 25.87 mL | 129.37 mL | 258.73 mL |
| 0.5 mM | 5.17 mL | 25.87 mL | 51.75 mL |
| 1 mM | 2.59 mL | 12.94 mL | 25.87 mL |
| 5 mM | 0.52 mL | 2.59 mL | 5.17 mL |
*The above data is based on the productmolecular weight 386.5 . 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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