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  4. Icaritin

Icaritin  (Synonyms: Anhydroicaritin)

Cat. No.: HY-N0678 Purity: 99.35%
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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.

Icaritin Chemical Structure

Icaritin Chemical Structure

CAS No. : 118525-40-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 86 In-stock
Solution
10 mM * 1 mL in DMSO USD 86 In-stock
Solid
1 mg USD 37 In-stock
5 mg USD 79 In-stock
10 mg USD 145 In-stock
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Based on 1 publication(s) in Google Scholar

Icaritin Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Icaritin

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3.

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.

Icaritin Related Antibodies

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
Molecular Weight

368.38

Formula

C21H20O6
CAS No.
Appearance

Solid

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
Structure Classification
Initial Source
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
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7146 mL 13.5729 mL 27.1459 mL
5 mM 0.5429 mL 2.7146 mL 5.4292 mL
View the Complete Stock Solution Preparation Table

* 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

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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:  15% Cremophor EL    85% Saline

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

  • Protocol 2

    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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline 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

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.35%

COA (250 KB) HNMR (274 KB) RP-HPLC (245 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Icaritin118525-40-9AnhydroicaritinAutophagyApoptosisInhibitorinhibitorinhibit

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