ARD-2585 | AR PROTAC | Probechem Biochemicals

Chemical Structure : ARD-2585

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ARD-2585 (ARD2585)

货号: PC-21125Not For Human Use, Lab Use Only.

ARD-2585 is a potent and orally bioavailable PROTAC androgen receptor (AR) degrader with DC50 of 0.04 nM, Dmax=99% in VCaP cell line.

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25 mg		Get quote
100 mg		Get quote

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生物&药学活性

ARD-2585 is a potent and orally bioavailable PROTAC androgen receptor (AR) degrader with DC50 of 0.04 nM, Dmax=99% in VCaP cell line.
ARD-2585 potently inhibits cell growth with IC50 values of 1.5 and 16.2 nM in the VCaP and LNCaP cell lines, respectively.
ARD-2585 is highly potent and effective in reducing the AR T878A mutant protein level in the LNCaP cell line with DC50 values of 0.1 nM and Dmax values of 98%.
ARD-2585 is >100 times more potent than enzalutamide in inhibition of VCaP cell growth, also >10 times more potent than ARV-110 in cell growth inhibition in the VCaP cell line.
ARD-2585 effectively reduces the AR protein in the VCaP tumor with a single oral administration (20 mg/kg, oral) in mice, effectively inhibits the AR protein level in tumor tissue.
ARD-2585 induces AR degradation through a cereblon-, proteasome-, and neddylation-dependent mechanism.
ARD-2585 at both 20 and 40 mg/kg is more efficacious than enzalutamide at 40 mg/kg in inhibition of tumor growth.

物理化学性质&存储条件

分子量	763.30
分子式	C41H43ClN8O5
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-((1r,4r)-4-((3-chloro-4-cyanophenyl)(methyl)amino)cyclohexyl)-4-(4-(1-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)azetidin-3-yl)piperazin-1-yl)benzamide

参考文献

1. Weiguo Xiang, et al. J Med Chem. 2021 Sep 23;64(18):13487-13509.

ARD-2585 (ARD2585)

生物&药学活性

物理化学性质&存储条件

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ARD-2585 (ARD2585)

生物&药学活性

物理化学性质&存储条件

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