SC428
Based on 1 Customer Validation
SC428 is an androgen receptor (AR) inhibitor that targets the N-terminal domain. SC428 potently decrease the transactivation of (AR)-V7, (AR)v567es, as well as full-length ( AR ) (AR-FL) and its LBD mutants, substantially. SC428 inhibits androgen-stimulated (AR)-FL nuclear translocation, chromatin binding, and (AR) -regulated gene transcription. SC428 inhibits the proliferation of tumor cells in vitro. SC428 inhibits tumor cell growth by inducing apoptosis in mice transplanted with 22RV1.
For research use only. We do not sell to patients.
- CAS No.: 1898232-70-6
- Formula: C15H10F3N3OS
- Molecular Weight:337.32
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
Biological Activity
Description
In Vitro
SC428 (10 nM- 1 μM, 48 h), which inhibits AR-V7 (IC50is 0.42 μM) and ARv567es (IC50 is 1.31 μM) activity in 293T (PSA-Luc)[1].
SC428 (5 μM, 5 h) reverses DHT-induced thermal stabilization of AR-FL (EC50 is 0.31 μM) in LNCaP (CETSA), inhibits ligand-induced activation of AR in a concentration-dependent manner and is an antagonist of the F887 L mutant[1].
SC428 (1, 2.5 and 5 μM, 30 min) inhibits the proliferation of LNCaP (IC50is 1.39 μM), VCaP (IC50 is 1.01 μM), 22RV1 (IC50 is 1.13 μM) AR-positive cell line. The ability of anti-proliferation is weak in AR-negative cell line PC3 (IC50 is 6.49 μM)[1].
SC428 (5 μM, 5 h) attenuates transcription of AR-regulated genes in LNCaP-AR cells (ChIP experiments) , blocks AR-FL chromatin binding (confocal imaging experiments) , and reduces nuclear translocation[1].
SC428 (2.5, 5 μmol/L, 24 h) inhibits AR signaling in prostate cancer cells that overexpress AR-V7[1].
SC428 (0.5, 1, 2.5 and 5 μM, 24 h) has inhibitory effects on both LNCaP-ARV7 and LNCaP- wt cells (Enzalutamide (HY-70002)-resistant), inhibiting PSA and UBE2C at both protein and mRNA levels (WB and qPCR) [1].
SC428 (5 μM, 5 h) disrupts AR-V7 dimer (immunoprecipitation assay) and nuclear localization (confocal imaging technique) in 22RV1 cells[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:LNCaP-AR
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Concentration:5 μmol/L
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Incubation Time:24 h
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Result:Inhibited AR-FL transcription significantly and rogen-mediated mRNA expression.
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Cell Line:22Rv1
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Concentration:2.5 and 5 μmol/L
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Incubation Time:24 h
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Result:2.5 mmol/L SC428 reduced AR-regulated gene mRNA to 50% of controls, whereas 5 mmol/L SC428 further reduced it to 10% to 30% of controls. AR-V7-dependent Ar signaling was blocked in 22Rv1 cells.
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Cell Line:LNCaP-AR-V7
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Concentration:0.5, 1, 2.5 and 5 μmol/L
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Incubation Time:24 h
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Result:Inhibited the expression of PSA gene in LNCaP-AR-V7 cells and significantly decreased the mRNA level of AR-V7 specific gene UBE2C.
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Cell Line:LNCaP-AR-V7
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Concentration:0.5, 1, 2.5 and 5 μmol/L
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Incubation Time:24 h
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Result:Inhibited PSA-Luc with equal potency in LNCaP-AR-V7 and LNCaP-ARWT cells.
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Cell Line:LNCaP-AR-V7，22Rv1
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Concentration:5 μmol/L
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Incubation Time:5 h
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Result:Reduced AR-V7 homodimer.
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Cell Line:LNCaP, VCaP, 22Rv1, PC3
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Concentration:1, 2.5 and 5 μmol/L
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Incubation Time:30 min
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Result:Inhibited the proliferation of three AR-positive cell lines, and the anti-proliferation effect of SC428 on the AR-negative cell line PC3 was 6-fold lower than that on the AR-positive cell line.
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Cell Line:LNCaP-AR
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Concentration:0.1 μM - 10 μM
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Incubation Time:30 h
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Result:Overcame the ENZ-resistant AR signaling and cell proliferation driven by AR-V7.
In Vivo
SC428 (90 mg/kg; intraperitoneal injection; five times a week; 3 weeks) inhibited the growth of AR-V7 in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:22Rv1 cells were subcutaneously injected into the right flank of male Nu/Nu mice[1].
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Dosage:60 mg/kg
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Administration:Intraperitoneal injection (i.p.) ; daily route 5 days a week; 3 weeks
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Result:Reduced the tumor growth by 50% , the mice did not lose weight, and the tumor PSA was reduced to undetectable levels.
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Animal Model:22Rv1 cells were subcutaneously injected into the right flank of male Nu/Nu mice. Male Nu/Nu mice were surgically castrated when the implanted 22Rv1 cells achieved an average tumor size of 200 mm3[1].
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Dosage:90 mg/kg
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Administration:Intraperitoneal injection (i.p.); daily route 5 days a week; 3 weeks
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Result:Inhibited the growth of prostate cancer with high expression of AR-V7.Good drug tolerance, no significant weight loss.
Chemical Information
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CAS No. 1898232-70-6
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Appearance Solid
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Molecular Weight 337.32
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Formula C15H10F3N3OS
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Color White to yellow
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SMILES
N#CC1=CC=C(NC(N/C=C/C2=CC=CS2)=O)C=C1C(F)(F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (296.45 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)
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. 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. 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 40% PEG300 5% Tween-80 45% 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 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.
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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Cytoplasmic-Nuclear Fractionated Protein Extraction
Cytoplasmic-nuclear fractionated protein extraction separates soluble cytoplasmic proteins from nuclear-enriched proteins by mild plasma-membrane permeabilization, differential centrifugation, washing of nuclei, and extraction of nuclear proteins for downstream immunoblotting or related molecular analysis. The readout is the relative abundance of a protein in cytoplasmic and nuclear fractions, commonly assessed by western blotting together with compartment markers such as tubulin or pyruvate kinase for cytoplasm and lamin, nucleoporin, hnRNP, H2AX, or Lamin B for nuclear fractions.
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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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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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Protocol for Cell Counting and Cell Density Analysis
Cell counting and cell-density analysis estimate the number of cells in a known volume or field area. Manual hemocytometer counting uses a chamber of defined geometry to convert counted cells into cells/mL, while automated counters and image-analysis workflows detect cell objects from optical, brightfield, fluorescence, impedance, or digital-image features. Trypan blue viability counting is based on dye exclusion: viable cells with intact membranes exclude dye, while non-viable cells with compromised membranes stain blue. The readout is total cell density, viable-cell density, dead-cell density, and percent viability. Cell density can also be estimated from microscopy images by counting objects per image area, from flow cytometry using calibrated volume or reference particles, or from in situ microscopy in bioreactors after calibration against reference methods such as hemocytometer or flow cytometry.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
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Somatic Cell Culture
A method of simulating the in vivo environment in vitro to maintain the cell growth, differentation and main functions.
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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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CCK-8/WST-8 Cell Proliferation Assay
The CCK-8/WST-8 assay is based on the reduction of the water-soluble tetrazolium salt WST-8 to a water-soluble formazan product by cellular dehydrogenases in metabolically active cells, where the generated formazan amount is proportional to the number of living cells and is quantified by measuring absorbance in the visible range, providing a colorimetric readout for cell viability and proliferation assessment. This class of tetrazolium-based assays improves upon earlier MTT-based systems by producing a water-soluble formazan, eliminating the need for organic solubilization steps and enabling direct spectrophotometric measurement in culture medium.
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Cell Counting-Based Growth Curve Assay
Cell counting-based growth curve assays quantify cell proliferation by directly measuring changes in viable cell number over time using manual or automated counting methods such as hemocytometer-based counting or instrument-assisted cell enumeration, enabling construction of growth curves that reflect population expansion dynamics in response to culture conditions. A widely used approach is trypan blue exclusion with hemocytometer counting, where membrane-compromised (non-viable) cells take up the dye, allowing discrimination between viable and non-viable cells while simultaneously enabling total cell number quantification. Repeated sampling across time points allows estimation of proliferation rate, growth phases, and comparative growth kinetics between experimental conditions.
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MTT Cell Proliferation Assay
The MTT assay is a colorimetric endpoint assay for estimating viable cell number, cell growth, cytotoxicity, or cell activation in cultured mammalian cells. Living cells reduce the yellow tetrazolium salt MTT into purple/blue formazan, while dead cells do not generate the same signal; the resulting color can be quantified with a multiwell spectrophotometer. MTT reduction is commonly interpreted as a readout of metabolic activity that often correlates with viable cell number, but it should not be treated as a direct cell-counting method unless the assay is optimized for the cell type and experimental condition. Studies show that MTT reduction can involve mitochondrial and non-mitochondrial reducing systems, and formazan may accumulate in intracellular lipid droplets rather than simply marking mitochondria.
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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 (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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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. 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 | 2.9645 mL | 14.8227 mL | 29.6454 mL | 74.1136 mL |
| 5 mM | 0.5929 mL | 2.9645 mL | 5.9291 mL | 14.8227 mL | |
| 10 mM | 0.2965 mL | 1.4823 mL | 2.9645 mL | 7.4114 mL | |
| 15 mM | 0.1976 mL | 0.9882 mL | 1.9764 mL | 4.9409 mL | |
| 20 mM | 0.1482 mL | 0.7411 mL | 1.4823 mL | 3.7057 mL | |
| 25 mM | 0.1186 mL | 0.5929 mL | 1.1858 mL | 2.9645 mL | |
| 30 mM | 0.0988 mL | 0.4941 mL | 0.9882 mL | 2.4705 mL | |
| 40 mM | 0.0741 mL | 0.3706 mL | 0.7411 mL | 1.8528 mL | |
| 50 mM | 0.0593 mL | 0.2965 mL | 0.5929 mL | 1.4823 mL | |
| 60 mM | 0.0494 mL | 0.2470 mL | 0.4941 mL | 1.2352 mL | |
| 80 mM | 0.0371 mL | 0.1853 mL | 0.3706 mL | 0.9264 mL | |
| 100 mM | 0.0296 mL | 0.1482 mL | 0.2965 mL | 0.7411 mL |
SC428 Related Classifications
HY-164373 Related Classifications
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