生物活性
SU5416 (Semaxanib)是一种有效和选择性的血管内皮生长因子(VEGF)受体蛋白酪氨酸激酶1/2抑制剂，也抑制其他酪氨酸激酶KIT, MET，FLT3和RET. SU5416抑制了表达Flt-1和KDR的人血管内皮细胞对VEGF的细胞迁移，也抑制了胎盘生长因子(PIGF)对细胞迁移的反应，PIGF是Flt-1的一种特异性配体。SU5416也以剂量依赖的方式抑制仅表达Flt-1的单核细胞的趋化作用。此外，SU5416被发现在体外抑制Flt-1的酪氨酸激酶对PIGF的反应。SU5416在体内有效抑制试剂盒活性时，按每周两次的时间表。
化学数据
| 分子量 | 238.28 |
| 分子式 | C15H14N2O |
| CAS号 | 204005-46-9 |
| 纯度 | 99.63% |
| 溶解性（25°C） | DMSO 20 mg/mL |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | C6, Calu 6, A375, A431, and SF767T |
| 方法 | Tumor Cell Lines and Growth Assays. The EPH4-VEGF cell line is a murine epithelial cell line engineered to overexpress murine VEGF. EPH4-VEGF cells were cultured in DMEM/F-12; C6 cells were cultured in Ham’s F-10 and A375, A431, and LNCAP cells in DMEM. All of these cultures were supplemented with 10% FBS and 2 mM L-glutamine. Calu 6 and SF767T cells were cultured in MEM supplemented with 10% FBS, 2 mM L-glutamine, 1 mM sodium pyruvate, and 0.1 mM MEM nonessential amino acids solution. C6, Calu 6, A375, A431, and SF767T were plated in their respective growth medium at 2 × 103 cells/100 μl/well in 96-well, flat-bottomed plates. SU5416 was serially diluted in media containing DMSO (<0.5%) and added to cultures of tumor cells 1 day after the initiation of culture. Cell growth was measured after 96 h using the sulforhodamine B method. IC50s were calculated by curve fitting using four-parameter analysis. |
| 浓度 | 0, 0.05, 0.5, 5, 50 μm |
| 处理时间 | 96 h |
| 动物实验 |
|---|
| 动物模型 | Female BALB/c nu/nu mice Intracolonic Xenograft Model |
| 配制 | DMSO |
| 剂量 | 25 mg/kg/day 50μl for 39 days |
| 给药处理 | i.p. bolus injection |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 4.1967 mL | 20.9837 mL | 41.9674 mL |
| 5 mM | 0.8393 mL | 4.1967 mL | 8.3935 mL |
| 10 mM | 0.4197 mL | 2.0984 mL | 4.1967 mL |
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