| 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-piperidinyl]-3-oxo-1-phenylpropyl]-4-hydroxy-1-[(2R)-3-methyl-2-(3-methyl-5-isoxazolyl)-1-oxobutyl]-, (2S,4R)- | [CAS]
2666951-70-6 | [Synonyms]
2-Pyrrolidinecarboxamide, N-[(1S)-3-[4-[2-[4-[[[trans-3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]amino]carbonyl]phenyl]ethynyl]-1-piperidinyl]-3-oxo-1-phenylpropyl]-4-hydroxy-1-[(2R)-3-methyl-2-(3-methyl-5-isoxazolyl)-1-oxobutyl]-, (2S,4R)- | [Molecular Formula]
C52H59ClN6O7 | [MOL File]
2666951-70-6.mol | [Molecular Weight]
915.51 |
| Chemical Properties | Back Directory | [Boiling point ]
1095.6±65.0 °C(Predicted) | [density ]
1.31±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
13.75±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
ARD-266 is a potent PROTAC Degrader (DC50 = 0.2 ~1 nM, IC50 = 1~6 nM). ARD-266 effectively induces degradation of AR protein in AR-positive (AR+) LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2?1 nM. ARD-266 is capable of reducing the AR protein level by >95% in these AR+ prostate cancer cell lines and effectively reduces ARregulated gene expression suppression. | [Uses]
ARD-266 is a highly potent and von Hippel-Lindau E3 ligase-based Androgen Receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM[1]. ARD-266 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. | [IC 50]
VHL | [References]
[1] Han X, et al. Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands. J Med Chem. 2019 Dec 26;62(24):11218-11231. DOI:10.1021/acs.jmedchem.9b01393 |
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