Danazol
Based on 4 publication(s) in Google Scholar
Danazol inhibits the proliferation of cancer cell MDA-MB-231 and MCF-7 with IC50 of 65 µg/mL and 31 µg/mL. Danazol arrests the cell cycle at G1 phase, induces apoptosis in MDA-MB-231 through PKCα signaling pathway.
For research use only. We do not sell to patients.
- Purity : 99.66%
- CAS No.: 17230-88-5
- Formula: C22H27NO2
- Molecular Weight:337.46
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Danazol
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
Biological Activity
Description
In Vitro
Danazol (0-100 μM, 18-72 h) inhibits the proliferation and the formation of capillary-like tubular structures in HUVECs[2].
Danazol (5-20 μM, 48 h) inhibits melanogenesis in B16 cell with an IC50 of 9.3 μM by post-transcriptionally inhibiting the expression of tyrosinase protein[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 17230-88-5
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Appearance Solid
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Molecular Weight 337.46
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Formula C22H27NO2
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Color White to off-white
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SMILES
C#C[C@]1(O)CC[C@@]2([H])[C@]3([H])CCC4=CC5=C(C=NO5)C[C@]4(C)[C@@]3([H])CC[C@@]21C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (4)
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Journal Impact Factor
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Most Recent
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Biotechnol Bioeng
An integrated biomimetic array chip for establishment of collagen-based 3D primary human hepatocyte model for prediction of clinical drug-induced liver injury. [Abstract]2021 Dec;118(12):4687-4698. PMID: 34478150 -
Cardiovasc Drugs Ther
Identifying the Dominant Contribution of Human Cytochrome P450 2J2 to the Metabolism of Rivaroxaban, an Oral Anticoagulant. [Abstract]2022 Feb;36(1):121-129. PMID: 33411110 -
Heliyon
Zhibai dihuang pill (ZBDH) exhibits therapeutic effects on idiopathic central sexual precocity in rats by modulating the gut microflora. [Abstract]2024 Apr 16;10(9):e29723. PMID: 38707434
Danazol purchased from MedChemExpress. Usage Cited in: Heliyon. 2024 Apr 16;10(9):e29723. [Abstract]
The rats were injected with Danazol on PND5 to induce the ICPP rat model of ICPP. The ICPP rats in the positive control group were further treated with ZBDH and GnRHa, respectively.
Danazol purchased from MedChemExpress. Usage Cited in: Heliyon. 2024 Apr 16;10(9):e29723. [Abstract]
As shown by the results, the vaginal opening of Danazol-induced ICPP rats occurred on the PND17, which was significantly earlier than that of normal control rats; however, ZBDH and GnRHa treatments could effectively delay the vaginal opening time of ICPP rats.
Danazol purchased from MedChemExpress. Usage Cited in: Heliyon. 2024 Apr 16;10(9):e29723. [Abstract]
The Danazol-induced idiopathic central precocious puberty (ICPP) rat model was successfully constructed and ZBDH increased the vaginal opening time. The normal estrus cycle was displayed.
Danazol purchased from MedChemExpress. Usage Cited in: Heliyon. 2024 Apr 16;10(9):e29723. [Abstract]
The results revealed that ZBDH and GnRHa could inhibit the increase of serum hormones in Danazol-induced ICPP rats.
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Res Sq
Sex differences in viral entry protein expression, host responses to SARS-CoV-2, and in vitro responses to sex steroid hormone treatment in COVID-19. [Abstract]2020 Dec 31:rs.3.rs-100914. PMID: 33173861
Solvent & Solubility
In Vitro:
DMSO : 25 mg/mL (74.08 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 20 mg/mL (59.27 mM; Need ultrasonic)
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 (7.41 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (5.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (20.0 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.
Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 2 mg/mL (5.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2 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 EtOH stock solution (20.0 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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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.
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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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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 (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
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Handling Instructions (2659 KB)
References
[1]. Thomas GW, et al., Effects of danazol on endothelial cell function and angiogenesis. Fertil Steril. 2007 Oct;88(4 Suppl):1065-70. [Content Brief]
[2]. Chang TS, Lin JJ. Inhibitory effect of danazol on melanogenesis in mouse B16 melanoma cells. Arch Pharm Res. 2010 Dec;33(12):1959-65. [Content Brief]
[3]. Deka SJ, et al., Danazol has potential to cause PKC translocation, cell cycle dysregulation, and apoptosis in breast cancer cells. Chem Biol Drug Des. 2017 Jun;89(6):953-963. [Content Brief]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| Ethanol / DMSO | 1 mM | 2.9633 mL | 14.8166 mL | 29.6331 mL | 74.0829 mL |
| 5 mM | 0.5927 mL | 2.9633 mL | 5.9266 mL | 14.8166 mL | |
| 10 mM | 0.2963 mL | 1.4817 mL | 2.9633 mL | 7.4083 mL | |
| 15 mM | 0.1976 mL | 0.9878 mL | 1.9755 mL | 4.9389 mL | |
| 20 mM | 0.1482 mL | 0.7408 mL | 1.4817 mL | 3.7041 mL | |
| 25 mM | 0.1185 mL | 0.5927 mL | 1.1853 mL | 2.9633 mL | |
| 30 mM | 0.0988 mL | 0.4939 mL | 0.9878 mL | 2.4694 mL | |
| 40 mM | 0.0741 mL | 0.3704 mL | 0.7408 mL | 1.8521 mL | |
| 50 mM | 0.0593 mL | 0.2963 mL | 0.5927 mL | 1.4817 mL | |
| DMSO | 60 mM | 0.0494 mL | 0.2469 mL | 0.4939 mL | 1.2347 mL |