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| 25mg |
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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
| 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].
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| 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].
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| 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. |
| 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 |
[1]. Zhu Jf, et al. Icaritin shows potent anti-leukemia activity on chronic myeloid leukemia in vitro and in vivo by regulating MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings. PLoS One. 2011;6(8):e23720.
[2]. Yao D, et al. Icaritin, an exogenous phytomolecule, enhances osteogenesis but not angiogenesis--an in vitro efficacy study. PLoS One. 2012;7(8):e41264. [3]. Guo Y, et al. An anticancer agent icaritin induces sustained activation of the extracellular signal-regulated kinase (ERK) pathway and inhibits growth of breast cancer cells. Eur J Pharmacol. 2011 May 11;658(2-3):114-22. |
| Molecular Formula |
C21H20O6
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| Molecular Weight |
368.385
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| Exact Mass |
368.126
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| CAS # |
118525-40-9
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| SMILES |
O1C(C2C([H])=C([H])C(=C([H])C=2[H])OC([H])([H])[H])=C(C(C2=C(C([H])=C(C(C([H])([H])/C(/[H])=C(\C([H])([H])[H])/C([H])([H])[H])=C12)O[H])O[H])=O)O[H]
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| Synonyms |
IcaritinAnhydroicaritin
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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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