Molecular Formula |
C21H20O6 |
Molar Mass |
368.38 |
Density |
1.359 |
Melting Point |
239℃ |
Boling Point |
582.0±50.0 °C(Predicted) |
Flash Point |
206.7℃ |
Solubility |
DMSO : 14 mg/mL (38.00 mM; Need ultrasonic and warming);H2O : < 0.1 mg/mL (insoluble) |
Vapor Presure |
3.82E-14mmHg at 25°C |
Appearance |
Yellow crystalline powder |
Color |
light yellow to dark yellow |
Maximum wavelength(λmax) |
368nm(MeOH)(lit.) |
pKa |
6.44±0.40(Predicted) |
Storage Condition |
2-8°C |
Refractive Index |
1.656 |
MDL |
MFCD22422519 |
Physical and Chemical Properties |
Yellow crystalline powder, soluble in methanol, ethanol, DMSO and other organic solvents, derived from epimedium. |
In vitro study |
Icaritin (4-64 µM; 48 hours; K562, imatinib-resistant cells and primary CML cells) treatment inhibits proliferation of K562, imatinib-resistant cells and primary CML cells . Icaritin (0-64 µM; 48 hours; K562 and primary cells) treatment induces K562 or primary cells apoptosis in an concentration dependent manner. Icaritin (32 µM; K562 cells) treatment increases cell population in the sub-G1 phase in K562 cells. Icaritin (0-64 µM; 48 hours; K562 cells) treatment inhibits MAPK/ERK/JNK downstream signaling and diminishes Jak2/Stat3/Akt expression. Icaritin treatment also significantly inhibits Bcl-2 protein expression and up-regulated Bax protein expression in K562 with a dose-dependent manner accompanied by the cleavage activation of caspase-3 or caspase-9, and a down-regulated expression of Apaf-1. Cell Proliferation Assay Cell Line: K562, imatinib-resistant cells and primary CML cells Concentration: 4 µM, 8 µM, 16 µM, 32 µM and 64 µM Incubation Time: 48 hours Result: Inhibited cell proliferation. Apoptosis Analysis Cell Line: K562 or primary cells Concentration: 0 µM, 4 µM, 8 µM, 16 µM, 32 µM and 64 µM Incubation Time: 48 hours Result: Induced K562 or primary cells apoptosis. Cell Cycle Analysis Cell Line: K562 cells Concentration: 32 µM Incubation Time: Result: Cell population in the sub-G1 phase was increased. Western Blot Analysis Cell Line: K562 cells Concentration: 0 µM, 4 µM, 8 µM, 16 µM, 32 µM and 64 µM Incubation Time: 48 hours Result: Inhibited MAPK/ERK/JNK downstream signaling and diminishes Jak2/Stat3/Akt expression. |
In vivo study |
Icaritin (4-8 mg/kg; intraperitoneal injection; daily; for 10 weeks; female NOD-SCID nude mice) treatment could prolong lifespan of NOD-SCID nude mice inoculated with K562 cells without suppression of bone marrow in mouse leukemia model. Animal Model: Female NOD-SCID nude mice (6-8 weeks old) with K562 cells Dosage: 4 mg/kg and 8 mg/kg Administration: Intraperitoneal injection; daily; for 10 weeks Result: Could prolong lifespan of NOD-SCID nude mice inoculated with K562 cells without suppression of bone marrow. |
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