生物活性
Icaritin (Anhydroicaritin) 是 Epimedium Genusis 的异戊二烯类黄酮衍生物,有效抑制 K562 细胞 (IC50 为 8 μM) 和原代 CML 细胞 (对 CML-CP 的 IC50 值为 13.4 μM,对 CML-BC 的 IC50 值为 18 μM) 的增殖。Icaritin 可以调节 MAPK/ERK/JNK 和 JAK2/STAT3/AKT 信号传导,并具有增强成骨的作用。
Tumor Challenge and Treatments
The orthotopic tumor model was established via a subcapsular intrahepatic injection of 5 × 105Hepa1–6 cells, suspended in 25 μL of 50% Basement Membrane Extract (Trevigen), into the left lobe of the liver of anesthetized 6–8 week old B6 mice. For the subcutaneous tumor model, 1 × 106Hepa1–6 or 2 × 105H22 cells suspended in 100 μL phosphate buffered saline (PBS) were injected subcutaneously into the right flank of B6 mice or BALB/c mice. A total of 5 days after tumor cell transplantation, when tumors were palpable or subcutaneous tumors reached 100 mm3, the mice were randomly divided into treatment groups. Icaritin treatment, was administered daily at 70 mg/kg by gavage for up to 3 weeks. Corn oil was used as the vehicle control. Anti-PD-1 antibody (clone RMP1-14; BioXCell) was administered at 10 mg/kg by intraperitoneal injection a total of three times at 3 day intervals. Once tumors were palpable, tumor growth was monitored every other day for 17 days using calipers. The survival time of tumor-bearing mice was recorded from the day of inoculation. The mice were sacrificed if the tumor diameter exceeded 1.5 cm or if the mice showed any signs of pain. Tumor volumes were calculated using the following formula: Volume = (length × width2)/2.
化学数据
分子量 | 368.38 |
分子式 | C21H20O6 |
CAS号 | 118525-40-9 |
纯度 | 100.0% |
溶解性(25°C) | DMSO 5 mg/mL (warmed) |
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 | 2.7146 mL | 13.5729 mL | 27.1459 mL |
5 mM | 0.5429 mL | 2.7146 mL | 5.4292 mL |
10 mM | 0.2715 mL | 1.3573 mL | 2.7146 mL |