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Chemical Structure : ARD-2585
Catalog No.: 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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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.
| M.Wt | 763.30 | |
| Formula | C41H43ClN8O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Weiguo Xiang, et al. J Med Chem. 2021 Sep 23;64(18):13487-13509.
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