Cat. No.: HY-N0678

Icaritin

(Synonyms: Anhydroicaritin)

8 Cited Publications

Customer Review

Based on 8 publication(s) in Google Scholar

Icaritin (Anhydroicaritin) is a prenylflavonoid derivative from Epimedium brevicornuMaxim. and potently inhibits 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 can regulate MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings, also enhances osteogenesis^[3.

For research use only. We do not sell to patients.

Purity: 99.06%
CAS No.: 118525-40-9
Formula: C₂₁H₂₀O₆
Molecular Weight:368.38

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Icaritin Chemical Structure

CAS No.: 118525-40-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (8)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

All JAK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>100 μM Compound: 1	Cytotoxicity against human A549 cells assessed as cell viability by MTT assay Cytotoxicity against human A549 cells assessed as cell viability by MTT assay	[PMID: 26079090]
COS-7	IC₅₀	2.2 μM Compound: 3	Inhibition of human recombinant PDE5A1 expressed in COS7 cells Inhibition of human recombinant PDE5A1 expressed in COS7 cells	[PMID: 18778098]
Hep 3B2	IC₅₀	0.9 μM Compound: ICT; 1	Antiproliferative activity against human Hep3B cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human Hep3B cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 36745506]
HepG2	IC₅₀	>10 μM Compound: ICT; 1	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 36745506]
MCF7	IC₅₀	7 μM Compound: 1	Cytotoxicity against human MCF7 cells assessed as cell viability by MTT assay Cytotoxicity against human MCF7 cells assessed as cell viability by MTT assay	[PMID: 26079090]
MDA-MB-435S	IC₅₀	24.9 μM Compound: 1	Cytotoxicity against human MDA-MB-435S cells assessed as cell viability by MTT assay Cytotoxicity against human MDA-MB-435S cells assessed as cell viability by MTT assay	[PMID: 26079090]
NCI/ADR-RES	IC₅₀	52.09 μM Compound: 3	Cytotoxicity against human MCF7/ADR cells after 72 hrs by MTT assay Cytotoxicity against human MCF7/ADR cells after 72 hrs by MTT assay	[PMID: 19523827]
RPMI-8226	IC₅₀	20.78 μM Compound: Icaritin	Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 34644502]
SMMC-7721	IC₅₀	>10 μM Compound: ICT; 1	Antiproliferative activity against human SMMC-7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human SMMC-7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 36745506]
Vero	IC₅₀	21.6 μM Compound: 1	Cytotoxicity against African green monkey Vero cells assessed as cell viability by MTT assay Cytotoxicity against African green monkey Vero cells assessed as cell viability by MTT assay	[PMID: 26079090]

In Vitro

Icaritin (4-64 μM; 48 hours; K562, imatinib-resistant cells and primary CML cells) treatment inhibits proliferation of K562, imatinib-resistant cells and primary CML cells ^[1].
Icaritin (0-64 μM; 48 hours; K562 and primary cells) treatment induces K562 or primary cells apoptosis in an concentration dependent manner^[1].
Icaritin (32 μM; K562 cells) treatment increases cell population in the sub-G1 phase in K562 cells^[1].
Icaritin (0-64 μM; 48 hours; K562 cells) treatment inhibits MAPK/ERK/JNK downstream signaling and diminishes Jak2/Stat3/Akt expression. Icaritin treatment also significantly inhibits Bcl-2 protein expression and up-regulated Bax protein expression in K562 with a dose-dependent manner accompanied by the cleavage activation of caspase-3 or caspase-9, and a down-regulated expression of Apaf-1^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

K562, imatinib-resistant cells and primary CML cells
Concentration:

4 µM, 8 µM, 16 µM, 32 µM and 64 µM
Incubation Time:

48 hours
Result:

Inhibited cell proliferation.

Apoptosis Analysis^[1]

Cell Line:

K562 or primary cells
Concentration:

0 µM, 4 µM, 8 µM, 16 µM, 32 µM and 64 µM
Incubation Time:

48 hours
Result:

Induced K562 or primary cells apoptosis.

Cell Cycle Analysis^[1]

Cell Line:

K562 cells
Concentration:

32 µM
Incubation Time:
Result:

Cell population in the sub-G1 phase was increased.

Western Blot Analysis^[1]

Cell Line:

K562 cells
Concentration:

0 µM, 4 µM, 8 µM, 16 µM, 32 µM and 64 µM
Incubation Time:

48 hours
Result:

Inhibited MAPK/ERK/JNK downstream signaling and diminishes Jak2/Stat3/Akt expression.

In Vivo

Icaritin (4-8 mg/kg; intraperitoneal injection; daily; for 10 weeks; female NOD-SCID nude mice) treatment could prolong lifespan of NOD-SCID nude mice inoculated with K562 cells without suppression of bone marrow in mouse leukemia model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female NOD-SCID nude mice (6-8 weeks old) with K562 cells^[1]
Dosage:

4 mg/kg and 8 mg/kg
Administration:

Intraperitoneal injection; daily; for 10 weeks
Result:

Could prolong lifespan of NOD-SCID nude mice inoculated with K562 cells without suppression of bone marrow.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 118525-40-9
Appearance Solid
Molecular Weight 368.38
Formula C₂₁H₂₀O₆
Color Light yellow to yellow
SMILES

O=C1C(O)=C(C2=CC=C(OC)C=C2)OC3=C(C/C=C(C)\C)C(O)=CC(O)=C13
Synonyms

Anhydroicaritin
Structure Classification
- Flavonoids
- Flavonols
- Phenols
- Polyphenols
Initial Source
- Endogenous metabolite
- Human Gut Microbiota Metabolites
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (8)

All Cell Proliferation/Viability AssayCell Imaging/StainingRT-PCRWBIHC

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Journal Impact Factor

Food Chem

Effects of sun drying combined with baking processes on the flavor quality of Chongqing Tuocha raw tea. [Abstract]

2025 Dec 30:497:146992. PMID: 41285060
Food Chem

Flavonoid-mediated metabolic underpinning quality variation in red bud-sport pear mutants. [Abstract]

2025 May 31:489:144992. PMID: 40466530
Int J Biol Macromol

Functional characterization of triokinase/FMN cyclase as a ferroptosis regulator and potential direct target of icaritin in hepatocellular carcinoma. [Abstract]

2026 Apr:358:151597. PMID: 41933761
Phytomedicine

Icaritin induces paraptosis in hepatocellular carcinoma cells by targeting BHLHE40 via endoplasmic reticulum stress and mitochondrial dysfunction. [Abstract]

2025 May 21:143:156870. PMID: 40424981

Icaritin purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 May 21:143:156870. [Abstract]

Icaritin (0–50 μM; 48 h) significantly inhibited the growth of Huh7, CRL8024, SNU449, and HepG2 hepatocellular carcinoma cells in a dose-dependent manner.

Icaritin purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 May 21:143:156870. [Abstract]

Icaritin (0–20 μM; 24 h) induced paraptotic cells in Huh7, CRL8024, SNU449, and HepG2 cell lines, with cytoplasmic vacuolation highlighted by red arrows.

Icaritin purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 May 21:143:156870. [Abstract]

qRT-PCR quantification of mRNA expression levels of key ER stress-responsive genes (PERK, ATF4, HSPA5, and DDIT3) in SNU449 cells was performed after treatment with Icaritin (5-30 μM; 4-8 h).

Icaritin purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 May 21:143:156870. [Abstract]

Icaritin (5-30 μM; 1-4 h) rapidly upregulated BHLHE40 expression in SNU449 and Huh7 cells, with levels increasing significantly in a dose- and time- dependent manner.

Icaritin purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 May 21:143:156870. [Abstract]

Immunohistochemical images and Quantification for Ki67 and BHLHE40 staining in Huh7 cell (sh-NTC and sh-BHLHE40)-derived xenografts of NOD SCID mice with or without Icaritin (75 mg/kg; i.g.; once daily for 14 d) treatment.
Int Immunopharmacol

Icaritin attenuates ischemia-reperfusion injury by anti-inflammation, anti-oxidative stress, and anti-autophagy in mouse liver. [Abstract]

2024 Jun 25:138:112533. PMID: 38924868
Biol Proced Online

Establishment of a mouse lung cancer organoid model and its applications for therapeutic screening. [Abstract]

2025 Jun 16;27(1):21. PMID: 40524168
J Pharm Pharmacol

Icariside I reduces breast cancer proliferation, apoptosis, invasion, and metastasis probably through inhibiting IL-6/STAT3 signaling pathway. [Abstract]

2024 May 3;76(5):499-513. PMID: 37971302
Int J Clin Pract Suppl

2026.

Solvent & Solubility

In Vitro:

DMSO : 15.62 mg/mL (42.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7146 mL

13.5729 mL

27.1459 mL

5 mM

0.5429 mL

2.7146 mL

5.4292 mL

10 mM

0.2715 mL

1.3573 mL

2.7146 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1.56 mg/mL (4.23 mM); Clear solution

This protocol yields a clear solution of ≥ 1.56 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (15.6 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 1.51 mg/mL (4.10 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 15% Cremophor EL 85% Saline

Solubility: 10 mg/mL (27.15 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7146 mL	13.5729 mL	27.1459 mL	67.8647 mL
	5 mM	0.5429 mL	2.7146 mL	5.4292 mL	13.5729 mL
	10 mM	0.2715 mL	1.3573 mL	2.7146 mL	6.7865 mL
	15 mM	0.1810 mL	0.9049 mL	1.8097 mL	4.5243 mL
	20 mM	0.1357 mL	0.6786 mL	1.3573 mL	3.3932 mL
	25 mM	0.1086 mL	0.5429 mL	1.0858 mL	2.7146 mL
	30 mM	0.0905 mL	0.4524 mL	0.9049 mL	2.2622 mL
	40 mM	0.0679 mL	0.3393 mL	0.6786 mL	1.6966 mL

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Icaritin

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Publications Citing Use of MedChemExpress (MCE) Icaritin

All JAK Isoforms

Biological Activity

Chemical Information

Publications (8)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Icaritin Related Classifications

Cat. No.: HY-N0678