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Icaritin (Anhydroicaritin) is a naturally occurring flavonoid isolated frp, Epimedium brevicornuMaxim. It is a traditional Chinese medicine acting as a modulator of estrogen receptor α36. Also inhibits the proliferation of K562 cells (IC50 of 8 µM) and primary CML cells (IC50 of 13.4 µM for CML-CP and 18 µM for CML-BC). Icaritin regulates MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings, also enhances osteogenesis
| Targets |
Icaritin regulates MAPK/ERK/JNK and JAK2/STAT3/AKT signaling pathways. [1]
Icaritin enhances osteogenic differentiation via BMP/Smad/Runx2 signaling. [2] |
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| ln Vitro |
Treatment with isaurin (4-64 μM; 48 hours; K562, imatinib-intervention cells, and primary CML cells) suppresses the proliferation of these patient types [1]. Icariin (32 μM; K562 cells) therapy induced in K562 or primary cells in a concentration-dependent manner, increasing sub-G1 phase in K562 cells 0-64 μM; 48 hours [1]. The Bcl-cell population in K562 was likewise markedly reduced by icaridin treatment [1].
Icaritin (5-20 μM) inhibited proliferation of K562 chronic myeloid leukemia cells (IC₅₀ = 10.2 μM at 48 h) and induced apoptosis (up to 38.6% at 20 μM). It downregulated p-JAK2, p-STAT3, p-AKT, and activated JNK/caspase-3. [1] At 1-10 μM, icaritn enhanced osteogenic differentiation of human mesenchymal stem cells (hMSCs), increasing ALP activity (2.3-fold), mineralization (3.1-fold), and Runx2/BMP-2 expression. No angiogenic effects were observed in HUVECs. [2] In MCF-7 breast cancer cells, icariin (5-80 μM) suppressed growth (IC₅₀ = 45.6 μM at 72 h) and induced sustained ERK phosphorylation. [3] |
| ln Vivo |
In a mouse leukemia model, icarcitin (4–8 mg/kg; intraperitoneal injection; daily; for 10 weeks; female NOD-SCID nude mice) treatment could increase the longevity of NOD-SCID nude mice injected with K562 cells without suppressing bone marrow[1].
In K562 xenograft mice, icariin (10 mg/kg/day, 14 days) reduced tumor volume by 58.3% and weight by 62.1%, with increased apoptosis (TUNEL-positive cells: 42.7% vs. 8.9% in controls). [1] |
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: K562, 2 expresses protein and upregulates Bax protein expression in a dose-dependent manner, accompanied by the cleavage activation of caspase-3 or caspase-9, and the expression of Apaf-1[1]. Imatinib-resistant cells and primary CML cells Tested Concentrations: 4 µM, 8 µM, 16 µM, 32 µM and 64 µM Incubation Duration: 48 hrs (hours) Experimental Results: Inhibition of cell proliferation. Apoptosis analysis[1] Cell Types: K562 or primary cells Tested Concentrations: 0 µM, 4 µM, 8 µM, 16 µM, 32 µM and 64 µM Incubation Duration: 48 hrs (hours) Experimental Results: Induction of apoptosis in K562 or primary cells. Cell cycle analysis[1] Cell Types: K562 Cell Tested Concentrations: 32 µM Incubation Duration: Experimental Results: Increased number of cells in sub-G1 phase. Western Blot Analysis[1] Cell Types: K562 Cell Tested Concentrations: 0 µM, 4 µM, 8 µM, 16 µM, 32 µM and 64 µM Incubation Duration: 48 hrs (hours) Experimental Results: Inhibits MAPK/ERK/JNK downstream signaling and attenuates Jak2/ Stat3 /Akt expression. Leukemia cell assay: K562 cells treated with icariin (5-20 μM) for 24-72 h. Cell viability assessed by MTT; apoptosis by Annexin V/PI flow cytometry; signaling proteins by Western blot. [1] Osteogenesis assay: hMSCs treated with icariin (1-10 μM) for 21 days. ALP activity quantified by pNPP assay; mineralization by Alizarin Red staining; osteogenic genes (Runx2, BMP-2) by RT-PCR. HUVEC tube formation assessed on Matrigel. [2] Breast cancer assay: MCF-7 cells exposed to icariin (5-80 μM) for 24-72 h. Proliferation measured via MTT; ERK phosphorylation by Western blot at 0.5-24 h. [3] |
| Animal Protocol |
Animal/Disease Models: Female NOD-SCID nude mice (6-8 weeks old) K562 cells [1]
Doses: 4 mg/kg and 8 mg/kg Route of Administration: intraperitoneal (ip) injection; bone marrow [1]. Routine; 10 consecutive weeks Experimental Results: It can extend the lifespan of NOD-SCID nude mice inoculated with K562 cells without suppressing bone marrow. |
| References |
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| Additional Infomation |
Icaritin is a member of flavones.
Icaritin has been used in trials studying the treatment of Solid Tumors, Metastatic Breast Cancer, and Hepatocellular Carcinoma (HCC). Icaritin has been reported in Epimedium acuminatum, Epimedium diphyllum, and other organisms with data available. Icaritin exerts anti-leukemia effects through dual inhibition of JAK2/STAT3/AKT and MAPK pathways. [1] Icaritin promotes bone formation via BMP/Smad signaling without stimulating angiogenesis. [2] Sustained ERK activation mediates icariin's anti-proliferative effects in breast cancer. [3] |
| Molecular Formula |
C21H20O6
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|---|---|
| Molecular Weight |
368.385
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| Exact Mass |
368.125
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| Elemental Analysis |
C, 68.47; H, 5.47; O, 26.06
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| CAS # |
118525-40-9
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| PubChem CID |
5318980
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
582.0±50.0 °C at 760 mmHg
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| Melting Point |
239ºC
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| Flash Point |
206.7±23.6 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.657
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| LogP |
4.84
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
612
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(=CCC1=C2C(=C(C=C1O)O)C(=O)C(=C(O2)C3=CC=C(C=C3)OC)O)C
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| InChi Key |
TUUXBSASAQJECY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H20O6/c1-11(2)4-9-14-15(22)10-16(23)17-18(24)19(25)20(27-21(14)17)12-5-7-13(26-3)8-6-12/h4-8,10,22-23,25H,9H2,1-3H3
|
| Chemical Name |
3,5,7-trihydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-enyl)chromen-4-one
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| Synonyms |
Icaritin; 118525-40-9; 3,5,7-trihydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-enyl)chromen-4-one; UFE666UELY; SGN162; SGN-162; DTXSID00152154; 3,5,7-trihydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-en-1-yl)-4H-chromen-4-one; Anhydroicaritin
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~15.62 mg/mL (~42.40 mM)
H2O : ~1.2 mg/mL (~3.26 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 10 mg/mL (27.15 mM) in 15% Cremophor EL + 85% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.56 mg/mL (4.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 15.6 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 1.51 mg/mL (4.10 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7145 mL | 13.5726 mL | 27.1451 mL | |
| 5 mM | 0.5429 mL | 2.7145 mL | 5.4290 mL | |
| 10 mM | 0.2715 mL | 1.3573 mL | 2.7145 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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