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ChemicalBook--->CAS DataBase List--->2316837-08-6

2316837-08-6

2316837-08-6 Structure

2316837-08-6 Structure
IdentificationBack 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
Chemical PropertiesBack Directory
[density ]

1.33±0.1 g/cm3(Predicted)
[form ]

Solid
[pka]

13.61±0.40(Predicted)
[color ]

White to light yellow
Hazard InformationBack 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.
[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
2316837-08-6 suppliers list
Company Name: Aladdin Scientific
Tel:
Website: www.aladdinsci.com/
Company Name: Shanghai?Medlife?Pharm-Tech?Co.,?Ltd  
Tel: 021-59167510 18117107507
Website: www.med-life.cn/
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