| Bioactivity | 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]. | |||||||||
| Invitro | ARD-61 binds to AR protein through its AR antagonist portion and von Hippel-Lindau (VHL)/cullin 2 E3 ligase through its VHL ligand portion to recruit AR protein to cullin 2 for ubiquitination, followed by proteasome-dependent AR degradation[1]. ARD-61 (0.001-100 μM; for 7 days) has IC50 values of 235 nM and 121 nM in the MDA-MB-453 and HCC1428 cell lines, which have the highest AR expression, respectively. ARD-61 demonstrates partial cell growth inhibition, delivering IC50 values of 39, 147, and 380 nM, respectively, in the MCF-7, BT-549 and MDA-MB-415 cell lines, which have a moderate level of AR protein[1]. ARD-61 (25-100000 nM; 6-72 h) induces G2/M cell cycle arrest in a dose- and time-dependent manner in each of these three AR+ breast cancer cell lines[1]. ARD-61 (25-100000 nM; 72 h) induces apoptosis in the MDA-MB-453 and HCC1428 cell lines[1]. ARD-61 (0.01-1000 nM; 6 h) is highly potent and effective in reducing AR protein levels. ARD-61 (0.01-1000 nM; 24 h) reduces the level of PR protein with a DC50 value of 0.15 nM in the T47D cells. ARD-61 has no obvious effect on ER and GR proteins[1]. ARD-61 (1 µM; for 24 h) effectively inhibits Wnt/β-catenin and MYC signaling pathways. ARD-61 (1-1000 nM; for 24 h) not only decreases both phosphorylated HER2 and HER3, but also un-phosphorylated HER2 and HER3 proteins[1]. Efficient knock-down of VHL completely blocks AR degradation induced by ARD-61 (100 nM; 24 h) in both MDA-MB-453 and MCF-7 cell lines[1]. Cell Viability Assay[1] Cell Line: | |||||||||
| Name | ARD-61 | |||||||||
| CAS | 2316837-08-6 | |||||||||
| Formula | C61H71ClN8O7S | |||||||||
| Molar Mass | 1095.78 | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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ARD-61
CAS: 2316837-08-6 F: C61H71ClN8O7S W: 1095.78
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectivel
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