ARD-2128 | AR PROTAC | Probechem Biochemicals

Chemical Structure : ARD-2128

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ARD-2128 (ARD2128)

货号: PC-21126Not For Human Use, Lab Use Only.

ARD-2128 is a potent, orally active PROTAC androgen receptor (AR) degrader with DC50 of 0.28 nM in CcaP cell line.

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生物&药学活性

ARD-2128 is a potent, orally active PROTAC androgen receptor (AR) degrader with DC50 of 0.28 nM in CcaP cell line.
ARD-2128 potently inhibits cell growth in the LNCaP cell line with IC50 of 5 nM.
ARD-2128 effectively suppresses the expression of PSA and TMPRSS2 genes in both VCaP and LNCaP cell lines in a dose-dependent manner, ARD-2128 is effective in reducing the mRNA levels of PSA and TMPRSS2 genes at 10 nM.
ARD-2128 (10-40 mg/kg, oral) exhibits antitumor efficacy in the VCaP xenograft tumor model in SCID mice.

物理化学性质&存储条件

分子量	820.39
分子式	C45H50ClN7O6
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	N-[trans-3-(3-Chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]-4-[4-[[1-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]-4-piperidinyl]methyl]-1-piperazinyl]benzamide

参考文献

1. Xin Han, et al. J Med Chem. 2021 Sep 9;64(17):12831-12854.

ARD-2128 (ARD2128)

生物&药学活性

物理化学性质&存储条件

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ARD-2128 (ARD2128)

生物&药学活性

物理化学性质&存储条件

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