Icaritin (Anhydroicaritin) is a flavonoid derivative of isoprene from Epimedium Genusis. It effectively inhibited the proliferation of K562 cells (IC50 8 µM) and primary CML cells (IC50 13.4 µM for CML-CP and 18 µM for CML-BC). Icaritin can regulate MAPK/ERK/JNK and JAK2/STAT3/AKT signaling and enhance osteogenesis.
Tumor Challenge and Treatments
The orthotopic tumor model was established via a subcapsular intrahepatic injection of 5 × 105 Hepa1–6 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 × 106 Hepa1–6 or 2 × 105 H22 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.
| Molecular Weight | 368.38 |
| Formula | C21H20O6 |
| CAS Number | 118525-40-9 |
| Solubility (25°C) | DMSO 5 mg/mL (warmed) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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