W6134
Based on 1 Customer Validation
W6134 is highly potent and selective RORγ covalent inhibitor with an IC50 of 0.21 μM. W6134 exhibits excellent selectivity for RORγ over RORα, RXRγ, and ERRγ. W6134 significantly inhibits RORγ transcriptional activity W6134 inhibits the proliferation and colony formation and induces apoptosis in castration-resistant prostate cancer cells (CRPC). W6134 can be used for the research of castration-resistant prostate cancers (CRPC).
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- Purity: 99.90%
- CAS No.: 2983540-55-0
- 화학식: C25H23ClN2O4S
- 분자량:482.98
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보관:Powder -20°C, 3 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
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Covalent Screening Library
HY-L036
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Transcription Factor-Targeted Library
HY-L090
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Anti-Prostate Cancer Compound Library
HY-L124
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Nuclear Receptor Compound Library
HY-L126
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Metabolic Enzyme Compound Library
HY-L146
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Highly Selective Inhibitors Library
HY-L158
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Highly Selective Activators Library
HY-L159
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Cell Death Library
HY-L162
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Anti-Drug-Resistant Compound Library
HY-L169
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Covalent Screening Library Plus
HY-L036P
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Bioactive Compound Library
HY-L001
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Protein Kinase Compound Library
HY-L196
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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High-Throughput Bioactive Compound Library
HY-L205
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Apoptosis Compound Library
HY-L003
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Metabolism/Protease Compound Library
HY-L012
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Anti-Cancer Compound Library
HY-L025
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Small Molecule Immuno-Oncology Compound Library
HY-L031
Biological Activity
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RORγ 0.21 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CWR22R | IC50 |
0.77 μM
Compound: 29
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Antiproliferative activity against human 22Rv1 cells incubated for 4 days by CCK8 assay
Antiproliferative activity against human 22Rv1 cells incubated for 4 days by CCK8 assay
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[PMID: 38227771] |
| LNCaP | IC50 |
0.63 μM
Compound: 29
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Antiproliferative activity against human LNCaP cells incubated for 4 days by CCK8 assay
Antiproliferative activity against human LNCaP cells incubated for 4 days by CCK8 assay
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[PMID: 38227771] |
| LNCaP C4-2B | IC50 |
0.47 μM
Compound: 29
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Antiproliferative activity against human LNCaP C4-2B cells incubated for 4 days by CCK8 assay
Antiproliferative activity against human LNCaP C4-2B cells incubated for 4 days by CCK8 assay
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[PMID: 38227771] |
W6134 (compound 29) has antiproliferative potencies on androgen receptor (AR)-positive human CRPC cell lines, including C4-2B, 22Rv1, and LNCaP, with IC50 values of 0.47 μM, 0.77 μM, and 0.63 μM, respectively[1].
W6134 (1.25-5 μM; 14 days) significantly suppresses the colony formation in C4-2B and 22Rv1 cell lines. W6134 dramatically induces apoptosis of C4-2B and 22Rv1 cells[1].
W6134 (1.25-5 μM; 48 h) inhibits the mRNA levels of AR-regulated genes, such as KLK2, KLK3, and NKX3-1[1].
W6134 (1.25-5 μM; 24-48 h) effectively suppresses the levels of AR or AR-V7 in a dose- and time-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:C4-2B and 22Rv1 cell lines
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Concentration:1.25 μM, 2.5 μM, 5 μM
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Incubation Time:14 days
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Result:Significantly suppressed the colony formation in C4-2B and 22Rv1 cell lines in a dose-dependent manner.
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Cell Line:C4-2B and 22Rv1 cell lines
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Concentration:1.25 μM, 2.5 μM, 5 μM
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Incubation Time:48 h
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Result:Significantly decreased the expression of AR and its variant AR-V7 in a dose-dependent manner.
The mRNA levels of AR-regulated genes, such as KLK2, KLK3, and NKX3-1, were also dramatically suppressed.
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Cell Line:C4-2B and 22Rv1 cell lines
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Concentration:1.25 μM, 2.5 μM, 5 μM
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Incubation Time:24 h, 48 h, 72 h
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Result:Effectively suppressed the levels of AR or AR-V7 in a dose- and time-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male NOD/SCID mice (~18 g; 4-week-old) were subcutaneously 22Rv1 cells[1]
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Dosage:5 mg/kg or 10 mg/kg
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Administration:i.p; five times per week; for 2 weeks
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Result:Significantly inhibited the tumor growth in a dose-dependent manner with tumor growth inhibition (TGI) values of 41.90 and 62.58% at doses of 5 and 10 mg/kg.
Chemical Information
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CAS No. 2983540-55-0
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Appearance Solid
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분자량 482.98
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화학식 C25H23ClN2O4S
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Color White to off-white
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SMILES
O=C(NC1=CC=C(C2=C(C=CC=C2)NC(C=C)=O)C(Cl)=C1)CC3=CC=C(C=C3)S(=O)(CC)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 83.33 mg/mL (172.53 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. 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)
순도&문서
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Data Sheet (275 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 | 2.0705 mL | 10.3524 mL | 20.7048 mL | 51.7620 mL |
| 5 mM | 0.4141 mL | 2.0705 mL | 4.1410 mL | 10.3524 mL | |
| 10 mM | 0.2070 mL | 1.0352 mL | 2.0705 mL | 5.1762 mL | |
| 15 mM | 0.1380 mL | 0.6902 mL | 1.3803 mL | 3.4508 mL | |
| 20 mM | 0.1035 mL | 0.5176 mL | 1.0352 mL | 2.5881 mL | |
| 25 mM | 0.0828 mL | 0.4141 mL | 0.8282 mL | 2.0705 mL | |
| 30 mM | 0.0690 mL | 0.3451 mL | 0.6902 mL | 1.7254 mL | |
| 40 mM | 0.0518 mL | 0.2588 mL | 0.5176 mL | 1.2940 mL | |
| 50 mM | 0.0414 mL | 0.2070 mL | 0.4141 mL | 1.0352 mL | |
| 60 mM | 0.0345 mL | 0.1725 mL | 0.3451 mL | 0.8627 mL | |
| 80 mM | 0.0259 mL | 0.1294 mL | 0.2588 mL | 0.6470 mL | |
| 100 mM | 0.0207 mL | 0.1035 mL | 0.2070 mL | 0.5176 mL |
W6134 Related Classifications
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