生物活性
MAZ51 is originally synthesized inhibitor of VEGFR-3 (Flt-4) tyrosine kinase, inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 also inhibited cellular proliferation by inducing G2/M phase cell cycle arrest without triggering significant cell death in dose- and time-dependent patterns. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Treatment of glioma cells with MAZ51 increased phosphorylated GSK3β levels by activating Akt and increasing levels of active RhoA.
In vivo, in the rats subcutaneously injected with MT450 rat mammary carcinoma cells, treatment daily with MAZ51 (8 mg/kg, i.p.) significantly suppressed the growth of MT450 tumors when compared with the solvent-treated animals. In the mammary fat pad of BALB/c mice injected with the metastatic mammary tumor cell line Cl66, MAZ51 treatment (i.p.) significantly inhibited tumor growth in a dose-dependent manner.
化学数据
| 分子量 | 314.38 |
| 分子式 | C21H18N2O |
| CAS号 | 163655-37-6 |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO ≥ 7 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 |
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 | 3.1809 mL | 15.9043 mL | 31.8086 mL |
| 5 mM | 0.6362 mL | 3.1809 mL | 6.3617 mL |
| 10 mM | 0.3181 mL | 1.5904 mL | 3.1809 mL |
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