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Chemical Structure| 118525-40-9 Chemical Structure| 118525-40-9

Structure of Icaritin
CAS No.: 118525-40-9

Chemical Structure| 118525-40-9

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Icaritin is a flavonoid that can enhance osteoblastic differentiation of mesenchymal stem cells (MSCs) and display a role of estrogen-like activities. Icaritin could be extracted from the roots of Epimedium brevicornu Maxim with anti-cancer effects.

Synonyms: Anhydroicaritin; Cycloicaritin

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Product Details of Icaritin

CAS No. :118525-40-9
Formula : C21H20O6
M.W : 368.38
SMILES Code : O=C1C(O)=C(OC2=C(C(O)=CC(O)=C12)C/C=C(C)\C)C3=CC=C(C=C3)OC
Synonyms :
Anhydroicaritin; Cycloicaritin
MDL No. :MFCD22422519
InChI Key :TUUXBSASAQJECY-UHFFFAOYSA-N
Pubchem ID :5318980

Safety of Icaritin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HT-29 cells 20 µM 36 hours Icaritin inhibited the formation of CDK2/cyclin E complex, reduced CDK2 activity, leading to attenuated phosphorylation of FOXO1, Rb, and P27, and E2F/Rb dissociation iScience. 2022 Aug 22;25(9):104991.
PLC cells 20 µM 36 hours Icaritin inhibited the formation of CDK2/cyclin E complex, reduced CDK2 activity, leading to attenuated phosphorylation of FOXO1, Rb, and P27, and E2F/Rb dissociation iScience. 2022 Aug 22;25(9):104991.
3T3-L1 cells 10^-6 M 10 days To investigate the effect of Icaritin on adipogenesis of 3T3-L1 cells. Results showed that Icaritin significantly inhibited lipid droplet formation and the expression of PPAR-γ and aP2. Biomaterials. 2015 Aug;59:125-43
Rabbit bone marrow mesenchymal stem cells (BMSCs) 10^-6 M 10 days To investigate the effect of Icaritin on osteogenic differentiation of BMSCs. Results showed that Icaritin significantly enhanced ALP activity and calcium nodule deposition, and promoted the expression of COL1α, OC, RUNX2, and BMP-2. Biomaterials. 2015 Aug;59:125-43
HIEC 0-60 μM 24 and 48 hours Lower toxicity on normal cells Adv Sci (Weinh). 2025 May;12(20):e2412953
MB49 9.32 μmol/L (IC50) 48 hours Evaluate the inhibitory effect of ICT on MB49 cell viability, showing that ICT significantly inhibits cancer cell viability. Acta Pharm Sin B. 2024 Sep;14(9):3916-3930
T24 19.55 μmol/L (IC50) 48 hours Evaluate the inhibitory effect of ICT on T24 cell viability, showing that ICT significantly inhibits cancer cell viability. Acta Pharm Sin B. 2024 Sep;14(9):3916-3930
UMUC-3 15.71 μmol/L (IC50) 48 hours Evaluate the inhibitory effect of ICT on UMUC-3 cell viability, showing that ICT significantly inhibits cancer cell viability. Acta Pharm Sin B. 2024 Sep;14(9):3916-3930
SW620 0-60 μM 24 and 48 hours Suppressed CRC cell survival in a dose- and time-dependent manner Adv Sci (Weinh). 2025 May;12(20):e2412953
HCT116 0-60 μM 24 and 48 hours Suppressed CRC cell survival in a dose- and time-dependent manner Adv Sci (Weinh). 2025 May;12(20):e2412953
DU145 cells 30 µM 48 hours Inhibited proliferation, migration, and invasion abilities of DU145 cells J Exp Clin Cancer Res. 2024 May 23;43(1):149
RM-1 cells 30 µM 48 hours Inhibited proliferation, migration, and invasion abilities of RM-1 cells J Exp Clin Cancer Res. 2024 May 23;43(1):149
RAW264.7 cells 1486.8 μg/L 48 hours Evaluate the effect of M@BPICT on inflammatory cytokine secretion in RAW264.7 cells, results showed that M@BPICT significantly reduced the proportion of LPS-stimulated M1 macrophages and the expression of inflammatory factors IL-6 and TNF-α J Nanobiotechnology. 2024 Mar 1;22(1):87
Bone marrow mesenchymal stem cells (BMSCs) 1486.8 μg/L 24, 48, 72, 120 hours Evaluate the cytotoxicity and proliferation effects of M@BPICT on BMSCs, results showed that M@BPICT exhibited good biocompatibility and promoted BMSCs proliferation J Nanobiotechnology. 2024 Mar 1;22(1):87

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Emu Steroid-associated osteonecrosis (SAON) model Implantation 320 mg Icaritin per 100 g PLGA/TCP Single implantation, observed for 12 weeks To evaluate the efficacy of P/T/I scaffold in preventing femoral head collapse in the SAON emu model. Results showed that the P/T/I group had a significantly lower incidence of femoral head collapse, better preserved cartilage thickness and mechanical properties, and more new bone formation within the bone tunnel. Biomaterials. 2015 Aug;59:125-43
C57BL/6 mice Subcutaneous RM-1 cell tumor model Intraperitoneal injection 10 mL/kg Five times a week for ICA, every two days for CUR, for 25 days Inhibited tumor growth and regulated gut microbiota and SCFAs J Exp Clin Cancer Res. 2024 May 23;43(1):149
Nude mice Hepatoma model Intraperitoneal injection 100 mg/kg Three times a week for four weeks Icaritin inhibits tumorigenesis of HepG2 cells in nude mice. J Exp Clin Cancer Res. 2021 Apr 1;40(1):118
Nude mice Hepatocellular carcinoma xenograft model Intraperitoneal injection 1.5 mg/kg Once every two days for 16 days Evaluate the anti-tumor effect of icaritin combined with CFH/OM-L on hepatocellular carcinoma xenograft model J Nanobiotechnology. 2022 Mar 5;20(1):114
C57BL/6J mice Subcutaneous tumor model Oral gavage 30 mg/kg Twice daily for 14 days Evaluate the inhibitory effect of ICT on subcutaneous tumor growth, showing that ICT significantly inhibits tumor growth and prolongs mouse survival. Acta Pharm Sin B. 2024 Sep;14(9):3916-3930
BALB/c nude mice Subcutaneous tumor model and lung metastasis model Intraperitoneal injection 35 mg/kg Twice a week for 3 weeks Evaluate the therapeutic effect of Icaritin combined with GP chemotherapy on ICC Adv Sci (Weinh). 2024 Apr;11(16):e2306174
Nude mice HCT116 subcutaneous xenograft model Intraperitoneal injection 40 and 80 mg/kg Once daily for 14 days Inhibited CRC cell proliferation in mice with no significant changes in body weight or organ damage Adv Sci (Weinh). 2025 May;12(20):e2412953

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01972672 Hepatocellular Carcinoma (HCC) PHASE2 COMPLETED 2025-03-17 Cancer institute & hospital, c... More >>hinese academy of medical sciences, Beijing, Beijing, 100021, China|Beijing Shenogen Biomedical Co., Ltd, Beijing, Beijing, 102206, China|NanJing PLA 81 Hospital, Nanjing, Jiangsu, 210002, China Less <<
NCT02496949 Solid Tumors PHASE1 COMPLETED 2025-08-13 Cancer institute & hospital, c... More >>hinese academy of medical sciences, Beijing, Beijing, 100021, China Less <<
NCT06285149 HCC PHASE2 NOT_YET_RECRUITING 2025-06-01 -
NCT01278810 Metastatic Breast Cancer PHASE1 UNKNOWN 2025-12-11 Cancer institute & hospital, c... More >>hinese academy of medical sciences, Beijing, Beijing, 100021, China Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.57mL

2.71mL

1.36mL

27.15mL

5.43mL

2.71mL

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