生物活性
Sunitinib Malate是一种多靶点RTK抑制剂，作用于VEGFR2 (Flk-1)和 PDGFRβ，也会抑制c-Kit的活性。用于治疗肾细胞癌（RCC）和伊马替尼耐药的胃肠道间质瘤（GIST）。
Targets
| Target | Value |
| Kit | | |
| FLT3 | | |
| PDGFRβ | IC50: 2nM |
| VEGFR2 | IC50: 80nM |
| FGFR1 | IC50: 2.9μM |
| EGFR | IC50: >20μM |
化学数据
| 目录号 | A10880 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 532.6 |
| Formula | C22H27FN4O2.C4H6O5 |
| 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. | 341031-54-7 |
| Synonyms | SU-11248 |
| SMILES | CCN(CC)CCNC(=O)C1=C(NC(=C1C)/C=C\2/C3=C(C=CC(=C3)F)NC2=O)C.C([C@@H](C(=O)O)O)C(=O)O |
溶解度
| In vitro (25°C) | DMSO | 13 mg/mL (24.41 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 4% 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 | 18.78 mL | 93.88 mL | 187.76 mL |
| 0.5 mM | 3.76 mL | 18.78 mL | 37.55 mL |
| 1 mM | 1.88 mL | 9.39 mL | 18.78 mL |
| 5 mM | 0.38 mL | 1.88 mL | 3.76 mL |
*The above data is based on the productmolecular weight 532.6 . 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.
