| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
| Targets |
Cyasterone targets the epidermal growth factor receptor, a receptor tyrosine kinase that plays a critical role in cell proliferation, differentiation, and survival. It acts as a natural EGFR inhibitor, blocking EGFR signaling and downstream pathways. By inhibiting EGFR, it induces apoptosis and cell cycle arrest in cancer cells.
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| ln Vitro |
Cyasterone is cytotoxic to a range of
Cyasterone is cytotoxic to a range of cancer cell lines. It inhibits the growth of A549 and MGC823 cells by regulating the EGFR signaling pathway. In A549 and MGC823 cells, Cyasterone inhibits cell proliferation in a dose-dependent manner at concentrations of 0, 20, 40, and 60 μg/ml over 24 hours. It inhibits the expression of p-EGFR, p-MEK, and p-mTOR. |
| ln Vivo |
In vivo, cyasterone (ip; 5 mg/kg, 10 mg/kg, and 15 mg/kg; 21 days) has antiproliferative properties and suppresses the growth of tumors xenografted with MGC823 cells while causing negligible physical weight changes [2].
Cyasterone has antiproliferative properties and suppresses the growth of tumors xenografted with MGC823 cells in vivo. In BALB/C-nu mouse MGC823 xenograft tumor models, Cyasterone administered intraperitoneally at doses of 5 mg/kg, 10 mg/kg, and 15 mg/kg for 21 days inhibits tumor growth while causing negligible physical weight changes. |
| Enzyme Assay |
Cyasterone is evaluated in cell-free kinase assays using purified EGFR. The compound is incubated with EGFR and ATP, and the inhibition of kinase activity is measured. IC50 values are determined to quantify the potency of EGFR inhibition. Selectivity is assessed by screening against a panel of kinases.
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| Cell Assay |
Cell viability assay [1]
Cell Types: A549 cells and MGC823 Cell Tested Concentrations: 0 μg/ml, 20 μg/ml, 40 μg/ml, 60 μg/ml Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of cell proliferation in a dose-dependent manner Way. Western Blot Analysis[1] Cell Types: A549 Cell Tested Concentrations: 0 μg/ml, 20 μg/ml, 40 μg/ml, 60 μg/ml Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of p-EGFR, p-MEK and p - mTOR expression. Cyasterone is assessed in cell-based assays using A549 and MGC823 cells. Cells are treated with Cyasterone at concentrations of 0, 20, 40, and 60 μg/ml for 24 hours. Cell proliferation is measured using cell viability assays. The expression of p-EGFR, p-MEK, and p-mTOR is measured using Western blot analysis. |
| Animal Protocol |
Animal/Disease Models: BALB/C-nu mouse MGC823 xenograft tumor [1]
Doses: 5 mg/kg, 10 mg/kg and 15 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Inhibited the growth of MGC823 xenograft tumor in vivo. Cyasterone is administered intraperitoneally in BALB/C-nu mouse MGC823 xenograft tumor models at doses of 5 mg/kg, 10 mg/kg, and 15 mg/kg for 21 days. Efficacy is assessed by measuring tumor growth inhibition and body weight changes. |
| ADME/Pharmacokinetics |
Cyasterone has a molecular weight of 520.65 and a molecular formula of C29H44O8. It has a CAS number of 17086-76-9. The compound is a white to off-white solid powder with a purity of ≥98%. It has a LogP of -0.25. It is soluble in DMSO. It should be stored at <+8°C in a dry and dark place.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for Cyasterone. The compound is for research use only and is not intended for human therapeutic use. It has been shown to cause negligible physical weight changes in animal models.
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| References | |
| Additional Infomation |
Cyasterone are steroidal lactones, 21-hydroxysteroids, 2β-hydroxysteroids, 3β-hydroxysteroids, 14α-hydroxysteroids, 20-hydroxysteroids, 6-oxosteroids, and phytodermal steroids. They have been reported in Cyathula capitata, Ajuga taiwanensis, and other organisms with relevant data.
Cyasterone is a natural EGFR inhibitor mainly extracted from Ajuga decumbens Thunb (Labiatae). It has a CAS number of 17086-76-9. It is also known as Cyasteron. It displays anti-proliferation effects by inducing apoptosis and cell cycle arrest. The compound is for research use only and has not been approved for clinical use. |
| Molecular Formula |
C29H44O9
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|---|---|
| Molecular Weight |
536.66
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| Exact Mass |
520.303
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| CAS # |
17086-76-9
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| PubChem CID |
119444
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
742.8±60.0 °C at 760 mmHg
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| Flash Point |
242.0±26.4 °C
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| Vapour Pressure |
0.0±5.6 mmHg at 25°C
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| Index of Refraction |
1.600
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| LogP |
-0.25
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
37
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| Complexity |
1010
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| Defined Atom Stereocenter Count |
13
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| SMILES |
C[C@H]1[C@@H]([C@H](OC1=O)C)C[C@H]([C@@](C)([C@H]2CC[C@@]3([C@@]2(CC[C@H]4C3=CC(=O)[C@H]5[C@@]4(C[C@@H]([C@@H](C5)O)O)C)C)O)O)O
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| InChi Key |
NEFYSBQJYCICOG-YSEUJXISSA-N
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| InChi Code |
InChI=1S/C29H44O8/c1-14-16(15(2)37-25(14)34)10-24(33)28(5,35)23-7-9-29(36)18-11-20(30)19-12-21(31)22(32)13-26(19,3)17(18)6-8-27(23,29)4/h11,14-17,19,21-24,31-33,35-36H,6-10,12-13H2,1-5H3/t14-,15+,16-,17-,19-,21+,22-,23-,24+,26+,27+,28+,29+/m0/s1
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| Chemical Name |
5-beta-Stigmast-7-en-26-oic acid, 2-beta,3-beta,14,20,22,28-hexahydroxy-6-oxo-, gamma-lactone, (22R,24S,25S,28R)-
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| Synonyms |
AI344890 AI3 44890 AI3-44890 Cyasterone
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~192.07 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.80 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.80 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8634 mL | 9.3169 mL | 18.6338 mL | |
| 5 mM | 0.3727 mL | 1.8634 mL | 3.7268 mL | |
| 10 mM | 0.1863 mL | 0.9317 mL | 1.8634 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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