Icaritin |
Catalog No.GC38096
One-Click Copy Product Info
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Icaritin is a natural prenylated flavonoid compound with anticancer activity.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 118525-40-9
Sample solution is provided at 25 µL, 10mM.
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Icaritin is a natural prenylated flavonoid compound with anticancer activity. Icaritin downregulates androgen receptor (AR) and AR splice variants (ARvs) through the aryl hydrocarbon receptor (AhR)-mediated ubiquitin-proteasome degradation pathway. This mechanism inhibits AR transcriptional activity and induces apoptosis in AR-positive prostate cancer cells. Based on the background that AR signaling regulates ACE2 and TMPRSS2 expression, Icaritin can be used for research related to prostate cancer and COVID-19[1-4].
In vitro, Icaritin (1-100μM) treatment for 48 hours significantly inhibited cell viability and induced tumor cell death in T24, UMUC-3, and MB49 cells[5]. Icaritin (2-8μM) treatment for 24-72 hours significantly suppressed cell proliferation, caused S-phase arrest, and induced apoptosis in Burkitt, Raji, and P3HR-1 cells[6]. Icaritin (1-50μM) treatment for 48-72 hours dose-dependently inhibited cell proliferation, induced apoptosis, and caused G2/M phase arrest in NK/T, SNK-10, and SNT-8 cells[7].
In vivo, ovariectomized female C57BL/6J mice injected intraperitoneally with MPTP were intragastrically administered 20mg/kg Icaritin for 14 consecutive days. Icaritin attenuated uterine atrophy, reduced midbrain cell apoptosis, increased femoral chondrocyte number, and improved whole-body bone mineral density to alleviate osteoporosis[8]. C57BL/6 mice inoculated with B16F10 cells were intragastrically administered 17.5-70mg/kg Icaritin for 16 consecutive days. Icaritin reduced tumor burden, induced tumor necrosis, and prolonged survival time[9]. CBA/J×DBA/2 mice with recurrent spontaneous abortion were orally given 1mg/kg-10mg/kg Icaritin daily from gestational day 0.5 for 13 consecutive days. Icaritin reduced embryo resorption rate, improved fetal survival rate, ameliorated decidual tissue morphology, and promoted decidualization[10].
References:
[1] Huong NT, Son NT. Icaritin: A phytomolecule with enormous pharmacological values. Phytochemistry. 2023 Sep;213:113772.
[2] Yang XJ, Xi YM, Li ZJ. Icaritin: A Novel Natural Candidate for Hematological Malignancies Therapy. Biomed Res Int. 2019 Mar 28;2019:4860268.
[3] Zhang C, Sui X, Jiang Y, et al. Antitumor effects of icaritin and the molecular mechanisms. Discov Med. 2020 Jan-Feb;29(156):5-16.
[4] Bi Z, Zhang W, Yan X. Anti-inflammatory and immunoregulatory effects of icariin and icaritin. Biomed Pharmacother. 2022 Jul;151:113180.
[5] Mou Z, Chen Y, Hu J, et al. Icaritin inhibits the progression of urothelial cancer by suppressing PADI2-mediated neutrophil infiltration and neutrophil extracellular trap formation. Acta Pharmaceutica Sinica B. 2024;14(9):3916-3930.
[6] Li Z, Yao C, Liu S, et al. Cytotoxic Effect of Icaritin and Its Mechanisms in Inducing Apoptosis in Human Burkitt Lymphoma Cell Line. BioMed Research International. 2014;2014:391512.
[7] Wu T, Wang S, Wu J, et al. Icaritin induces lytic cytotoxicity in extranodal NK/T-cell lymphoma. Journal of Experimental & Clinical Cancer Research. 2015 Feb 15;34:17.
[8] Lin X, Zhou X, Liu X, et al. Icaritin alleviates motor impairment and osteoporosis in Parkinson's disease mice via the ER-PI3K/Akt pathway. Scientific Reports. 2025 Jan 25;15:3190.
[9] Hao H, Zhang Q, Zhu H, et al. Icaritin promotes tumor T-cell infiltration and induces antitumor immunity in mice. European Journal of Immunology. 2019;00:1-10.
[10] Huang S, Xia L, Xia Y, et al. Icaritin attenuates recurrent spontaneous abortion in mice by modulating Treg/Th17 imbalance via TGF-β/SMAD signaling pathway. BBA-Molecular Cell Research. 2024;1871:119574.
| Cell experiment [1]: | |
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Cell lines |
Raji cells (human Burkitt lymphoma cell line); P3HR-1 cells (human Burkitt lymphoma cell line) |
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Preparation Method |
Raji and P3HR-1 cells were maintained in RPMI 1640 medium supplemented with 10% heat-inactivated newborn calf serum at 37°C, 5% CO2. Cells were treated with Icaritin at 2-8μM for 24-72h. MTT assay, flow cytometry for cell cycle and apoptosis, and Western blot were performed. |
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Reaction Conditions |
2-8μM; 24-72h |
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Applications |
Icaritin significantly inhibited proliferation of Raji and P3HR-1 cells in a dose- and time-dependent manner. Icaritin caused S-phase arrest and induced apoptosis in Raji cells with activation of caspase-8 and caspase-9 and cleavage of PARP. Icaritin downregulated c-Myc and Bcl-2 and upregulated Bax in Raji cells. |
| Animal experiment [2]: | |
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Animal models |
C57BL/6 mice (male and female, 6-8 weeks old) |
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Preparation Method |
Mice were subcutaneously inoculated with B16F10 melanoma cells (2×106) or MC38 colorectal cells (5×105) on day 0. From day 3 to day 18 (B16F10) or day 20 (MC38) after inoculation, mice were orally gavaged with Icaritin at 17.5-70mg/kg body weight once daily. Tumor volume, tumor weight, survival, histopathology, tumor-infiltrating immune cells (flow cytometry), CD8 T-cell depletion (anti-CD8 mAb 10mg/kg i.p. twice weekly), combination with IL-2 (200μg/kg i.p. twice weekly) or anti-PD-1 (5mg/kg)/anti-CTLA-4 (10mg/kg) (i.p. twice weekly) were assessed. |
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Dosage form |
17.5-70mg/kg; p.o.; daily for 16 days or 18 days |
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Applications |
Icaritin decreased B16F10 melanoma and MC38 colorectal tumor burden and weight, induced tumor necrosis, prolonged survival, increased CD8 T-cell infiltration and proliferation with elevated effector memory frequency in tumors, reduced CD11b+Gr1+ MDSC frequency and PD-L1 expression on MDSCs and neutrophils in tumor microenvironment, and enhanced antitumor effect when combined with IL-2 or anti-PD-1/CTLA-4 blockade; CD8 T-cell depletion abolished the tumor growth inhibition. |
References: [1] Li Z, Yao C, Liu S, et al. Cytotoxic effect of icaritin and its mechanisms in inducing apoptosis in human Burkitt lymphoma cell line. BioMed Research International. 2014;2014:391512. [2] Hao H, Zhang Q, Zhu H, et al. Icaritin promotes tumor T-cell infiltration and induces antitumor immunity in mice. Eur J Immunol. 2019;00:1-10. | |
| Cas No. | 118525-40-9 | SDF | |
| Canonical SMILES | O=C1C(O)=C(C2=CC=C(OC)C=C2)OC3=C(C/C=C(C)\C)C(O)=CC(O)=C13 | ||
| Formula | C21H20O6 | M.Wt | 368.38 |
| Solubility | DMSO: 14 mg/mL (38.00 mM and warming); Water: < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7146 mL | 13.5729 mL | 27.1459 mL |
| 5 mM | 542.9 μL | 2.7146 mL | 5.4292 mL |
| 10 mM | 271.5 μL | 1.3573 mL | 2.7146 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)