Chemical Structure : W6134
CAS No.:
2983540-55-0
W6134
(RORγ covalent inhibitor 29)
Catalog No.: PC-21716Not For Human Use, Lab Use Only.
W6134 (RORγ covalent inhibitor 29) is a first-in-class, potent and selective RORγ covalent inhibitor with IC50 of 0.21 uM, targets the Cys320 of RORγ.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
W6134 (RORγ covalent inhibitor 29) is a first-in-class, potent and selective RORγ covalent inhibitor with IC50 of 0.21 uM, targets the Cys320 of RORγ.
W6134 displays no activities against RORα, RXRγ, and ERRγ (IC50>20 uM).
W6134 significantly suppresses the colony formation in C4-2B and 22Rv1 cell lines, dramatically induces apoptosis of C4-2B and 22Rv1 cells.
W6134 effectively inhibits RORγ-dependent transcriptional activity and RORγ-related gene transcription in CRPC cell lines.
W6134 (5 or 10 mg/kg, i.p.) demonstrates in vivo antitumor activity in 22RV1 cell-derived xenograft.
Physicochemical Properties
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M.Wt
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482.98
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Formula
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C25H23ClN2O4S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-(2'-Chloro-4'-(2-(4-(ethylsulfonyl)phenyl)acetamido)-[1,1'-biphenyl]-2-yl)acrylamide
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References
1. Wei Fang, et al. J Med Chem. 2024 Jan 16. doi: 10.1021/acs.jmedchem.3c02063.
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