ET516 | AR inhibitor | Probechem Biochemicals

Chemical Structure : ET516

CAS No.: 2820120-95-2

ET516 (ET-516)

Catalog No.: PC-20115Not For Human Use, Lab Use Only.

ET516 is a potent androgen receptor liquid-liquid phase separation (AR LLPS) inhibitor, specifically disrupts AR condensates, effectively suppresses AR transcriptional activity and inhibits the proliferation and tumor growth of prostate cancer cells expressing AR-resistant mutants.

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Biological Activity

ET516 is a potent androgen receptor liquid-liquid phase separation (AR LLPS) inhibitor, specifically disrupts AR condensates, effectively suppresses AR transcriptional activity and inhibits the proliferation and tumor growth of prostate cancer cells expressing AR-resistant mutants.

ET516 dose-dependently inhibited the ARE reporter activity and condensate formation of AR(F877L/T878A) with IC50 of 0.7 μM and 0.2 μM, respectively.

ET516 potently inhibited the phase separation capability and transcriptional activation of AR(WT), AR(T878A) and AR(W742C) without inducing nuclear translocation of AR or affecting AR protein levels.

ET516, but not enzalutamide, also suppressed the puncta formation and transcriptional activity of constitutively active AR splice variant AR(V7).

ET516 (10 uM) specifically reduced AR transcriptional activity and inhibits growth of CRPC, reduced the proliferation of AR-positive LNCaP and VCaP cells, but not that of AR-negative PC3 cells.

ET516 efficiently inhibited the growth of both enzalutamide-resistant mutants AR(F877L/T878A), and AR(V7) expressing cells, but not enzalutamide.

ET516 (30mg/kg, p.o., BID) reduced tumor growth of LNCaP-AR(F877L/T878A) xenografts.

Physicochemical Properties

M.Wt	529.44
Formula	C25H22Cl2N4O3S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(5-((4-(2-(3-chloro-4-(2-chloroethoxy)-5-cyanophenyl)propan-2-yl)phenyl)ethynyl)pyrimidin-2-yl)methanesulfonamide

References

1. Jingjing Xie, et al. Nat Chem Biol. 2022 Dec;18(12):1341-1350.

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ET516 (ET-516)

Biological Activity

Physicochemical Properties

References

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