生物活性
Vatalanib (PTK787) 2HCl是一种小分子蛋白激酶抑制剂,可抑制抑制所有已知VEGF受体以及血小板衍生的生长因子受体β和c-kit的血管生成,但对VEGFR-2的选择性最高。
Targets
| Target | Value |
| VEGFR2/KDR | IC50: 37nM |
| VEGFR1/FLT1 | IC50: 77nM |
| VEGFR2/Flk1 | IC50: 270nM |
| PDGFRβ | IC50: 580nM |
| VEGFR3/FLT4 | IC50: 660nM |
| c-Kit | IC50: 730nM |
| c-Fms | IC50: 1.4μM |
化学数据
| 目录号 | A10967 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 419.7 |
| Formula | C20H17Cl3N4 |
| 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. | 212141-51-0 |
| Synonyms | Vatalanib,PTK787,PTK/ZK |
| SMILES | C1=CC=C2C(=C1)C(=NN=C2NC3=CC=C(C=C3)Cl)CC4=CC=NC=C4.Cl.Cl |
溶解度
| In vitro | DMSO | 77 mg/mL (183.45 mM) |
| Water | 9 mg/mL (21.44 mM) |
| Ethanol | 5 mg/mL (11.91 mM) |
*<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 | 23.83 mL | 119.13 mL | 238.27 mL |
| 0.5 mM | 4.77 mL | 23.83 mL | 47.65 mL |
| 1 mM | 2.38 mL | 11.91 mL | 23.83 mL |
| 5 mM | 0.48 mL | 2.38 mL | 4.77 mL |
*The above data is based on the productmolecular weight 419.7 . 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.