生物活性
TSU-68 (Orantinib,SU6668)在无细胞试验中具有8 nM的Ki对PDGFR自磷酸化的最大效力，但也强烈抑制Flk-1和FGFR1反磷酸化，对IGF-1R，Met，Src， Lck，Zap70，Abl和CDK2； 不抑制EGFR。
靶点信息
| PDGFRβ (Cell-free assay) | FGFR1 (Cell-free assay) | Flk1 (Cell-free assay) | | |
| 8 nM(Ki) | 1.2 μM(Ki) | 2.1 μM(Ki) | | |
化学数据
| 目录号 | A10953 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 310.4 |
| Formula | C18H18N2O3 |
| 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. | 252916-29-3 |
| Synonyms | TSU68 |
| SMILES | CC1=C(NC(=C1CCC(=O)O)C)/C=C\2/C3=CC=CC=C3NC2=O |
溶解度
| In vitro (25°C) | DMSO | 55 mg/mL (177.22 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 1% DMSO+30% polyethylene glycol+1% Tween 80 | 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 | 32.22 mL | 161.08 mL | 322.16 mL |
| 0.5 mM | 6.44 mL | 32.22 mL | 64.43 mL |
| 1 mM | 3.22 mL | 16.11 mL | 32.22 mL |
| 5 mM | 0.64 mL | 3.22 mL | 6.44 mL |
*The above data is based on the productmolecular weight 310.4 . 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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