ARD-2128 是高效的雄激素受体降解剂PROTAC。它可有效降低 雄激素受体蛋白并抑制肿瘤组织中雄激素受体调节的基因，在没有毒性迹象的情况下抑制肿瘤生长。它有用于前列腺癌研究的价值。

ARD-2128 is a highly potent, orally bioavailable PROTAC degrader of androgen receptor (AR). ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer.

ARD-2128 is highly potent and effective in the inhibition of cell growth in the VCaP cell line and LNCaP cell line with the IC 50 values of 4 nM and 5 nM, respectively [1]. ARD-2128 (1, 10, 100, and 1000 nM; 24 hours; in VCaP cell) effectively reduces the AR protein level by >50% at 1 nM and achieves the AR degradation of >90% at 10, 100, and 1000 nM, respectively[1] . Cell Viability Assay [1] Cell Line: VCaP cell Concentration: 1, 10, 100, and 1000 nM Incubation Time: 24 hours Result: Reduces the AR protein level and achieves the AR degradation.

ARD-2128 (20 mg/kg; p.o.; once) is effective in reducing the level of AR protein in mice after 24 hours [1]. ARD-2128 (10-40 mg/kg; p.o.; daily for 21 days) shows antitumor activity in the VCaP xenograft model in mice [1] . ARD-2128 (5mg/kg; p.o.) treatment shows the C max , AUC 0-t and t 1/2 values of 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively [1] . Animal Model: SCID mice [1] Dosage: 20 mg/kg Administration: Oral Result: Reducing the level of AR protein in mice after 24 hours. Animal Model: SCID mice [1] Dosage: 10, 20, and 40 mg/kg Administration: P.o.; daily for 21 days Result: Inhibits tumor growth by 46, 69, and 63%, respectively. Animal Model: Male ICR Mice [1] Dosage: 5 mg/kg Administration: P.o. (Pharmacokinetic Analysis) Result: The C max , AUC 0-t and t 1/2 were 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively. ARD-2128 achieves 67% oral bioavailability in mice, effectively reduces AR protein and suppresses AR-regulated genes in tumor tissues with oral administration, leading to the effective inhibition of tumor growth in mice without signs of toxicity.

2222111-87-5

C45H50ClN7O6

820.39

DMSO:100 mg/mL (121.90 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years