| Identification | Back Directory | [Name]
2-Pyrrolidinecarboxamide, N-[(1S)-3-[4-[2-[4-[[[trans-3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]amino]carbonyl]phenyl]ethynyl][1,4'-bipiperidin]-1'-yl]-1-[4-(4-methyl-5-thiazolyl)phenyl]-3-oxopropyl]-4-hydroxy-1-[(2R)-3-methyl-2-(3-methyl-5-isoxazolyl)-1-oxobutyl]-, (2S,4R)- | [CAS]
2316837-08-6 | [Synonyms]
ARD-61
2-Pyrrolidinecarboxamide, N-[(1S)-3-[4-[2-[4-[[[trans-3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]amino]carbonyl]phenyl]ethynyl][1,4'-bipiperidin]-1'-yl]-1-[4-(4-methyl-5-thiazolyl)phenyl]-3-oxopropyl]-4-hydroxy-1-[(2R)-3-methyl-2-(3-methyl-5-isoxazolyl)-1-oxobutyl]-, (2S,4R)- | [Molecular Formula]
C61H71ClN8O7S | [MOL File]
2316837-08-6.mol | [Molecular Weight]
1095.78 |
| Hazard Information | Back Directory | [Description]
ARD-61 is an AR antagonist and PROTAC AR degrader. | [Uses]
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice[1]. ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. | [in vivo]
ARD-61 (25, 50?mg/kg/day; ip; for 75 days) effectively inhibits tumor growthin the MDA-MB-453 xenograft tumor model in male SCID mice[1].
ARD-61 (25?mg/kg; ip; single dose) effectively and rapidly reduces the AR protein in the MDA-MB-453 xenograft tissue, with the effect persisting for at least 24?h. ARD-61 is very effective in reducing the mRNA level of WNT7B in a time-dependent manner[1].
| Animal Model: | MDA-MB-453 xenograft tumor model in male SCID mice[1] | | Dosage: | 25, 50?mg/kg | | Administration: | IP; daily; for 75 days | | Result: | Effectively inhibited tumor growth.
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| [IC 50]
VHL | [References]
[1] Lijie Zhao, et al. A highly potent PROTAC androgen receptor (AR) degrader ARD-61 effectively inhibits AR-positive breast cancer cell growth in vitro and tumor growth in vivo. Neoplasia. 2020 Oct;22(10):522-532. DOI:10.1016/j.neo.2020.07.002 |
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