Bioactivity | ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models[1]. |
Invitro | ARD-1676 在 AR+ VCaP 和 LNCaP 细胞系中降解 AR 的 DC50 值分别为 0.1 和 1.1 nM,在 VCaP 和 LNCaP 细胞系中的 IC50 值分别为 11.5 和 2.8 nM[1]。 0 --> ARD-1676 相关抗体: |
In Vivo | ARD-1676 在小鼠、大鼠、狗和猴子中的口服生物利用度分别为 67%、44%、31% 和 99%。ARD-1676 可有效降低小鼠 VCaP 肿瘤组织中 AR 蛋白的水平,并抑制 VCaP 小鼠异种移植肿瘤模型中的肿瘤生长[1]。 |
Name | ARD-1676 |
CAS | 2632305-36-1 |
Formula | C44H46ClN7O5 |
Molar Mass | 788.33 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Xiang W, et al. Discovery of ARD-1676 as a Highly Potent and Orally Efficacious AR PROTAC Degrader with a Broad Activity against AR Mutants for the Treatment of AR + Human Prostate Cancer. J Med Chem. 2023 Sep 8.. |