ARD-1676 | AR PROTAC | Probechem Biochemicals

Chemical Structure : ARD-1676

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ARD-1676 (ARD1676, ARD 1676)

货号: PC-21160Not For Human Use, Lab Use Only.

ARD-1676 (ARD1676) is a highly potent and orally efficacious PROTAC degrader of the androgen receptor (AR) with DC50 values of 0.1 and 1.1 nM in AR+ VCaP and LNCaP cell lines, respectively.

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生物&药学活性

ARD-1676 (ARD1676) is a highly potent and orally efficacious PROTAC degrader of the androgen receptor (AR) with DC50 values of 0.1 and 1.1 nM in AR+ VCaP and LNCaP cell lines, respectively.
ARD-1676 effectively induces degradation of a broad panel of clinically relevant AR mutants with DC50 of 8 nM and Dmax > 95% in the MDA-Pca-2b cell line with AR double mutations (L702H and T878A), but not ARV-110 (Cat# PC-38047).
ARD-1676 exhibits cell growth inhibition in the VCaP and LNCaP cell line cell line with IC50 of 11.5 nM and 18.5 nM, respectively.
ARD-1676 effectively degrades >50% of the AR after a 1 h treatment time and achieved maximum degradation with a 3-6 h treatment time in both the VCaP and LNCaP cell lines at 10 and 100 nM.
ARD-1676 is highly effective and potent in reducing the K388R-, V716M-, W742C-, H875Y-, F877L-, and T878A-mutated AR proteins at concentrations as low as 1 nM, also effectively depletes two AR mutants with Δ388–390 and Δ873–879 deletion, respectively, but much less effective for reducing the levels of AR L702H- and S889G-mutated AR proteins.
ARD-1676 is a selective AR degrader among the >5500 proteins.
ARD-1676 (10-40 mg/kg, oral gavage daily for a total of 21 days) exhibits antitumor activity in the VCaP xenograft tumor model in SCID mice.

物理化学性质&存储条件

分子量	788.35
分子式	C44H46ClN7O5
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-chloro-4-((3S)-8-(4-(4-((6-(2,6-dioxopiperidin-3-yl)-5,7-dioxo-3,5,6,7-tetrahydropyrrolo[3,4-f]isoindol-2(1H)-yl)methyl)piperidine-1-carbonyl)phenyl)-3-methyl-2,8-diazaspiro[4.5]decan-2-yl)benzonitrile

参考文献

1. Weiguo Xiang, et al. Journal of Medicinal Chemistry 2023.

ARD-1676 (ARD1676, ARD 1676)

生物&药学活性

物理化学性质&存储条件

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ARD-1676 (ARD1676, ARD 1676)

生物&药学活性

物理化学性质&存储条件

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