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.
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- Purity: 98.0%
- CAS No.: 1898232-70-6
- 화학식: C15H10F3N3OS
- 분자량:337.32
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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.
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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.
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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분자량 337.32
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
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)
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.
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.
순도&문서
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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 |
|---|---|---|---|---|---|
| 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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