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ARD-1676 is an orally administered androgen receptor (AR) PROTAC degrader that combines an AR ligand with a cereblon ligand. It demonstrates AR-degrading activity both in vitro and in vivo, and effectively inhibits VCaP tumor growth in mouse xenograft models [1].
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5 mg | Inquiry | Backorder | |
50 mg | Inquiry | Backorder |
Description | ARD-1676 is an orally administered androgen receptor (AR) PROTAC degrader that combines an AR ligand with a cereblon ligand. It demonstrates AR-degrading activity both in vitro and in vivo, and effectively inhibits VCaP tumor growth in mouse xenograft models [1]. |
In vitro | ARD-1676 exhibits a DC50 for androgen receptor (AR) degradation at 0.1 nM in AR+ VCaP cells and 1.1 nM in LNCaP cell lines, while its IC50 values for inhibiting cell proliferation are 11.5 nM in VCaP and 2.8 nM in LNCaP cell lines [1]. |
In vivo | ARD-1676 exhibits oral bioavailability of 67%, 44%, 31%, and 99% in mice, rats, dogs, and monkeys, respectively. It effectively reduces AR (AR) protein levels in murine VCaP tumor tissues and inhibits tumor growth in the VCaP murine xenograft tumor model [1]. |
Molecular Weight | 788.33 |
Formula | C44H46ClN7O5 |
Cas No. | 2632305-36-1 |
Storage | Shipping with blue ice. |
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