2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. EGFR Apoptosis
  4. Cyasterone

Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors.

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Cyasterone Chemical Structure

Cyasterone Chemical Structure

CAS No. : 17086-76-9

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Based on 1 publication(s) in Google Scholar

Other Forms of Cyasterone:

Cyasterone Related Antibodies

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1 Publications Citing Use of MCE Cyasterone

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors[1].

IC50 & Target

IC50: EGFR[1]
In Vitro

Cyasterone exerts cytotoxicity on multiple cell lines: HeLa (IC50=77.24 μg/ml); HepG-2 (IC50=52.03 μg/ml); MCF-7 (IC50=82.07 μg/ml) and MCF-7 (IC50=82.07 μg/ml). And It has none cytotoxicity (IC50>400 μg/ml) on 3 types of carcinoma (HT-29, Caco-2, T47D) and 1 type of normal (NIH 3T3) cell lines[1].
Cyasterone (0-60 μg/ml; 48 hours) causes a significantly decreasing of the cell proliferation. It inhibits cell growth as a dose-dependent manner, exhibits IC50 values of 38.50 μg/ml and 32.96 μg/ml, respectively[1].
Cyasterone (0-60 μg/ml; 24 hours) decreases p-EGFR, p-MEK, and p-mTOR as a dose-dependent manner in A549 cells, it affects the MAPK signaling pathway activities[1].

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

Cyasterone Related Antibodies

Cell Viability Assay[1]

Cell Line: A549 cells and MGC823 cells
Concentration: 0 μg/ml, 20 μg/ml, 40 μg/ml, 60 μg/ml
Incubation Time: 24 hours
Result: Inhibited cell proliferation as a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 0 μg/ml, 20 μg/ml, 40 μg/ml, 60 μg/ml
Incubation Time: 24 hours
Result: Surpressed p-EGFR, p-MEK, and p-mTOR expression.
In Vivo

Cyasterone (intraperitoneal injection; 5 mg/kg, 10 mg/kg and 15 mg/kg; 21 days) has anti-proliferation effect in vivo and inhibits MGC823 cells xenografted tumor growth in vivo with few changes in body weights[2].

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

Animal Model: MGC823 xenograft tumor in BALB/C-nu mice[1]
Dosage: 5 mg/kg, 10 mg/kg and 15 mg/kg
Administration: Intraperitoneal injection
Result: Inhibited MGC823 xenograft tumor growth in vivo.
Molecular Weight

520.65

Formula

C29H44O8
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@]12[C@]([C@](C)([C@H](O)C[C@@H]3[C@@H](C)OC([C@H]3C)=O)O)([H])CC[C@@]1(O)C4=CC([C@]5([H])C[C@@H](O)[C@@H](O)C[C@]5(C)[C@@]4([H])CC2)=O
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (192.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9207 mL 9.6034 mL 19.2068 mL
5 mM 0.3841 mL 1.9207 mL 3.8414 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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: 99.58%

COA (253 KB) HNMR (126 KB) RP-HPLC (174 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9207 mL 9.6034 mL 19.2068 mL 48.0169 mL
5 mM 0.3841 mL 1.9207 mL 3.8414 mL 9.6034 mL
10 mM 0.1921 mL 0.9603 mL 1.9207 mL 4.8017 mL
15 mM 0.1280 mL 0.6402 mL 1.2805 mL 3.2011 mL
20 mM 0.0960 mL 0.4802 mL 0.9603 mL 2.4008 mL
25 mM 0.0768 mL 0.3841 mL 0.7683 mL 1.9207 mL
30 mM 0.0640 mL 0.3201 mL 0.6402 mL 1.6006 mL
40 mM 0.0480 mL 0.2401 mL 0.4802 mL 1.2004 mL
50 mM 0.0384 mL 0.1921 mL 0.3841 mL 0.9603 mL
60 mM 0.0320 mL 0.1601 mL 0.3201 mL 0.8003 mL
80 mM 0.0240 mL 0.1200 mL 0.2401 mL 0.6002 mL
100 mM 0.0192 mL 0.0960 mL 0.1921 mL 0.4802 mL
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Cyasterone 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:

Cyasterone17086-76-9EGFRApoptosisEpidermal growth factor receptorErbB-1HER1CANCERA549MGC823APOPTOSISInhibitorinhibitorinhibit

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