Art. -Nr.: HY-163192

W6134

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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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Reinheit: 99.90%
CAS. Nr.: 2983540-55-0
Formel: C₂₅H₂₃ClN₂O₄S
Molecular Weight:482.98

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

W6134 Chemical Structure

CAS. Nr.: 2983540-55-0

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

RORγ

0.21 μM (IC₅₀)

Alle ROR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CWR22R	IC₅₀	0.77 μM Compound: 29	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	[PMID: 38227771]
LNCaP	IC₅₀	0.63 μM Compound: 29	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	[PMID: 38227771]
LNCaP C4-2B	IC₅₀	0.47 μM Compound: 29	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	[PMID: 38227771]

In Vitro

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.

Cell Migration Assay ^[1]

Cell Line:

C4-2B and 22Rv1 cell lines
Concentration:

1.25 μM, 2.5 μM, 5 μM
Incubation Time:

14 days
Result:

Significantly suppressed the colony formation in C4-2B and 22Rv1 cell lines in a dose-dependent manner.

RT-PCR^[1]

Cell Line:

C4-2B and 22Rv1 cell lines
Concentration:

1.25 μM, 2.5 μM, 5 μM
Incubation Time:

48 h
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.

Western Blot Analysis^[1]

Cell Line:

C4-2B and 22Rv1 cell lines
Concentration:

1.25 μM, 2.5 μM, 5 μM
Incubation Time:

24 h, 48 h, 72 h
Result:

Effectively suppressed the levels of AR or AR-V7 in a dose- and time-dependent manner.

In Vivo

W6134 (compound 29) (5-10 mg/kg; i.p; five times per week; for 2 weeks) markedly suppresseS the tumor growth in a 22Rv1 mouse tumor xenograft model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male NOD/SCID mice (~18 g; 4-week-old) were subcutaneously 22Rv1 cells^[1]
Dosage:

5 mg/kg or 10 mg/kg
Administration:

i.p; five times per week; for 2 weeks
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

CAS. Nr. 2983540-55-0
Appearance Solid
Molecular Weight 482.98
Formel C₂₅H₂₃ClN₂O₄S
Color White to off-white
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0705 mL

10.3524 mL

20.7048 mL

5 mM

0.4141 mL

2.0705 mL

4.1410 mL

10 mM

0.2070 mL

1.0352 mL

2.0705 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Fang W, et al. Discovery of the First-in-Class RORγ Covalent Inhibitors for Treatment of Castration-Resistant Prostate Cancer. J Med Chem. 2024 Jan 16. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.0705 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

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W6134

Covalent Screening Library

Transcription Factor-Targeted Library

Anti-Prostate Cancer Compound Library

Nuclear Receptor Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Drug-Resistant Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Apoptosis Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Small Molecule Immuno-Oncology Compound Library

Alle ROR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

W6134

Covalent Screening Library

Transcription Factor-Targeted Library

Anti-Prostate Cancer Compound Library

Nuclear Receptor Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Drug-Resistant Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Apoptosis Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Small Molecule Immuno-Oncology Compound Library

Alle ROR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

W6134 Related Classifications

HY-163192 Related Classifications