Cyasterone
Based on 4 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity : 99.58%
- CAS No.: 17086-76-9
- Formula: C29H44O8
- Molecular Weight:520.65
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Cyasterone
MoreAll EGFR Isoforms
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Biological Activity
Description
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. Further protocols information, click here.
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Cell Line:A549 cells and MGC823 cells
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Concentration:0 μg/ml, 20 μg/ml, 40 μg/ml, 60 μg/ml
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Incubation Time:24 hours
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Result:Inhibited cell proliferation as a dose-dependent manner.
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Cell Line:A549 cells
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Concentration:0 μg/ml, 20 μg/ml, 40 μg/ml, 60 μg/ml
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Incubation Time:24 hours
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Result:Surpressed p-EGFR, p-MEK, and p-mTOR expression.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MGC823 xenograft tumor in BALB/C-nu mice[1]
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Dosage:5 mg/kg, 10 mg/kg and 15 mg/kg
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Administration:Intraperitoneal injection
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Result:Inhibited MGC823 xenograft tumor growth in vivo.
Chemical Information
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CAS No. 17086-76-9
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Appearance Solid
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Molecular Weight 520.65
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Formula C29H44O8
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Color White to off-white
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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
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Structure Classification
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (4)
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Journal Impact Factor
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Most Recent
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J Ethnopharmacol
The protective mechanism of Tao Hong Si Wu decoction against breast cancer through regulation of EGFR/ERK1/2 signaling. [Abstract]2024 Oct 5:332:118339. PMID: 38777083 -
Curr Med Chem
Cyasterone Improves Mitochondrial Function and Protects against Knee Osteoarthritis by Activating PPARγ. [Abstract]2026 Mar 5. PMID: 41837479 -
PLoS One
hUMSCs-exo@Cyasterone protects the cell model of steroid-induced femur head necrosis by regulating N-glycosylation modification of CTSD-N258A. [Abstract]2026 Apr 3;21(4):e0337562. PMID: 41931502 -
Anticancer Res
Gossypol Inhibits GLI3-dependent SHH Signaling to Selectively Target SPOP-deficient Breast Cancer Cells. [Abstract]2026 May;46(5):2317-2327. PMID: 42049345
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocols
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Flow cytometric DNA-content cell-cycle staining
Flow cytometric DNA-content cell-cycle staining measures the fluorescence intensity of DNA-bound fluorochromes in single cells or nuclei to estimate DNA content distributions, allowing assignment of populations to G0/G1, S, and G2/M phases by DNA histogram deconvolution. Propidium iodide (PI) intercalates into DNA, and PI fluorescence is proportional to cellular DNA content when staining is performed under conditions that make DNA accessible and minimize non-DNA signal. Cells with G2/M DNA content are expected to show approximately twice the fluorescence intensity of G0/G1 cells, while S-phase cells occupy intermediate fluorescence values. PI-based DNA-content analysis can also detect cells with fractional DNA content, often reported as sub-G1, when DNA fragmentation and extraction during staining reduce retained DNA signal in apoptotic cells. DAPI is an alternative DNA fluorochrome for univariate DNA-content analysis, while bivariate approaches combining DNA content with proliferation
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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BrdU Incorporation Assay
Bromodeoxyuridine (BrdU) incorporation assay is based on the principle that BrdU, a thymidine analog, is incorporated into newly synthesized DNA during the S phase of the cell cycle, thereby serving as a marker of DNA replication and cellular proliferation. Incorporated BrdU can be detected using anti-BrdU antibodies following DNA denaturation, enabling visualization or quantification of proliferating cells through immunochemical detection methods such as immunofluorescence or immunohistochemistry.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Protocol for Cell Cycle
Cell-cycle analysis by flow cytometry measures DNA content in single cells to estimate the fraction of cells in G0/G1, S, and G2/M phases. Propidium iodide intercalates into DNA, and after RNA removal with RNase, fluorescence intensity reflects cellular DNA content: 2N cells are assigned to G0/G1, cells between 2N and 4N to S phase, and 4N cells to G2/M. DNA-content analysis alone cannot reliably separate G0 from G1 or G2 from M. Ki-67 can distinguish quiescent G0 cells from cycling cells, EdU or BrdU incorporation marks active DNA synthesis in S phase, and phospho-histone H3 staining identifies mitotic cells within the 4N population.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Lu X, et al. Anti-proliferation effects, efficacy of cyasterone in vitro and in vivo and its mechanism. Biomed Pharmacother. 2016 Dec;84:330-339. [Content Brief]
[2]. Lu X,et al. Anti-proliferation effects, efficacy of cyasterone in vitro and in vivo and its mechanism.Biomed Pharmacother. 2016 Dec;84:330-339. [Content Brief]
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 |
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| 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 |
Cyasterone Related Classifications
HY-N0211 Related Classifications
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