Icaritin (Anhydroicaritin) |
| Catalog No.GC32762 |
Icaritin (Anhydroicaritin) is a natural flavonoid compound extracted from the traditional Chinese medicine Epimedium. Icaritin (Anhydroicaritin) is often used in research in the fields of anti-cancer, bone protection, anti-inflammation, neuroprotection, cardiovascular protection, and antiviral.
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 (Anhydroicaritin) is a natural flavonoid compound extracted from the traditional Chinese medicine Epimedium. Icaritin (Anhydroicaritin) is often used in research in the fields of anti-cancer, bone protection, anti-inflammation, neuroprotection, cardiovascular protection, and antiviral[1-9].
Icaritin (Anhydroicaritin)(0-40μM; 24h) induced mitophagy and apoptosis to provoke immunogenic cell death (ICD) both in mouse Hepa1–6 and human Huh7 HCC cells[1]. Icaritin (Anhydroicaritin) (10μM; 24h) reduces the levels of mature SREBP2 and its target genes in RANKL-induced osteoclasts in RAW264.7 cells[2]. Icaritin (Anhydroicaritin) (2-3μM; 24h) inhibits cell cycle arrest at the G2/M phase, accompanied by down-regulation of the expression levels of G2/M regulatory proteins (such as cyclin B, cdc2, and cdc25C), and strongly inhibits the growth of breast cancer MDA-MB-453 and MCF7 cells[3]. Icaritin (Anhydroicaritin) (5-50µM; 24h) increased the Bax/Bcl-2 ratio and caspase-3 activation in HepG2 cells, while Icaritin (Anhydroicaritin) stimulated c-Jun N-terminal kinase 1 (JNK1) but not JNK2, ERK1/2, and p38 subgroups of the mitogen-activated protein kinase (MAPK) family[4].
In a high-fat diet (HFD)-induced transgenic prostate adenocarcinoma mouse model, Icaritin (Anhydroicaritin) (30mg/kg; ip; 30 weeks) can inhibit the progression of prostate cancer in TRAMP mice by suppressing proinflammatory cytokines[5]. In the cyclophosphamide-induced bone marrow hematopoietic suppression mouse model, Icaritin (Anhydroicaritin) (10mg/kg; po; 5d) can improve bone marrow suppression by improving the bone marrow hematopoietic microenvironment, promoting the proliferation and differentiation of HSCs, inhibiting the apoptosis of HSCs, and stimulating the expression of G-CSF and TPO[6]. In the mouse B16F10 melanoma model and MC38 colorectal cancer model, Icaritin (Anhydroicaritin) (35mg/kg; po; 25d) inhibited the reduction of MDSCs frequency at tumor sites and enhanced T cell-mediated anti-tumor immunity[7]. In the senescence accelerated mouse 8 (SAMP8) mouse model, Icaritin (Anhydroicaritin) (75mg/kg; po; 22d) reduced Aβ production by decreasing BACE1 expression in the hippocampus of SAMP8 mice, thereby improving the memory and learning abilities of mice[8]. In a cerebral ischemia-reperfusion mouse model, Icaritin (Anhydroicaritin) (60mg/kg; ip; Pre-treatment 1h prior) treatment ameliorates acute cerebral ischemia-reperfusion injury by ameliorating apoptotic neuronal cell death, ROS/RNS-induced lipid peroxidation, ECM accumulation, and EndMT-related fibrosis in the mouse brain[9].
References:
[1]. Yu Z, Guo J, Hu M, et al. Icaritin exacerbates mitophagy and synergizes with doxorubicin to induce immunogenic cell death in hepatocellular carcinoma[J]. ACS nano, 2020, 14(4): 4816-4828.
[2]. Zheng Z G, Zhang X, Zhou Y P, et al. Anhydroicaritin, a SREBPs inhibitor, inhibits RANKL-induced osteoclastic differentiation and improves diabetic osteoporosis in STZ-induced mice[J]. European Journal of Pharmacology, 2017, 809: 156-162.
[3]. Guo Y M, Zhang X T, Meng J, et al. An anticancer agent icaritin induces sustained activation of the extracellular signal-regulated kinase (ERK) pathway and inhibits growth of breast cancer cells[J]. European journal of pharmacology, 2011, 658(2-3): 114-122.
[4]. He J, Wang Y, Duan F, et al. Icaritin induces apoptosis of HepG2 cells via the JNK1 signaling pathway independent of the estrogen receptor[J]. Planta medica, 2010, 76(16): 1834-1839.
[5]. Hu J, Yang T, Xu H, et al. A novel anticancer agent icaritin inhibited proinflammatory cytokines in TRAMP mice[J]. International urology and nephrology, 2016, 48: 1649-1655.
[6]. Sun C, Yang J, Pan L, et al. Improvement of icaritin on hematopoietic function in cyclophosphamide-induced myelosuppression mice[J]. Immunopharmacology and Immunotoxicology, 2018, 40(1): 25-34.
[7]. Hao H, Zhang Q, Zhu H, et al. Icaritin promotes tumor T‐cell infiltration and induces antitumor immunity in mice[J]. European Journal of Immunology, 2019, 49(12): 2235-2244.
[8]. Li Y Y, Huang N Q, Feng F, et al. Icaritin improves memory and learning ability by decreasing BACE‐1 expression and the Bax/Bcl‐2 ratio in senescence‐accelerated mouse prone 8 (SAMP8) mice[J]. Evidence‐Based Complementary and Alternative Medicine, 2020, 2020(1): 8963845.
[9]. Wu C T, Chen M C, Liu S H, et al. Bioactive flavonoids icaritin and icariin protect against cerebral ischemia–reperfusion-associated apoptosis and extracellular matrix accumulation in an ischemic stroke mouse model[J]. Biomedicines, 2021, 9(11): 1719.
| Cell experiment [1]: | |
Cell lines | Murine 4T1 cells and MDA-MB-231 cells |
Preparation Method | 4T1 and MAD-MB-231 cells (5×103/well) were separately seeded into 96-well plates. After 24h, the culture medium was replaced with fresh medium containing various concentrations of Icaritin (Anhydroicaritin)(0, 5, 10, 20, 40, 80, and 160µM). After incubation for 24h, cell viability was detected by MTT assay. |
Reaction Conditions | 0, 5, 10, 20, 40, 80, and 160µM; 24h |
Applications | The survival rates of 4T1 and MDA-MB-231 cells gradually decreased with the increase of Icaritin (Anhydroicaritin) concentration. The IC50 value of Icaritin (Anhydroicaritin) in MDA-MB-231 cells and 4T1 cells was 278.68μM and 319.83μM respectively at 24h. |
| Animal experiment [2]: | |
Animal models | Nude mice of human TNBC cell line xenografts |
Preparation Method | Six-week-old female nude mice were anesthetized, and the human TNBC cell line MDA-MB-231 (1×107) premixed with Matrigel at a ratio of 1:1 was subcutaneously injected into the fourth pair of breast fat pads on the left side of each mouse. When the tumor approximately grew to 5×5mm, the mice were randomized into the control group and Icaritin (Anhydroicaritin) group (20mg/kg). Mice received Icaritin (Anhydroicaritin) treatment by intraperitoneal injection once every 2 days for 4 weeks. |
Dosage form | 20mg/kg; ip; every 2 days for 4 weeks |
Applications | Icaritin (Anhydroicaritin) enhances GPX1 expression and inhibits EMT in the BC xenograft mouse model. |
References: | |
| 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) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
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 ddH2O, 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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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