ARD-2128 是一种高效的 PROTAC 雄激素受体(AR)降解剂。ARD-2128 可有效降低 AR 蛋白并抑制肿瘤组织中 AR 调节的基因，在没有毒性迹象的情况下抑制肿瘤生长。ARD-2128 作用在前列腺癌的研究上。
| 生物活性 | ARD-2128 is a highly potent, orally bioavailablePROTACandrogen receptor(AR)degrader. 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 prostatecancer[1]. |
| IC50& Target | IC50: 4 nM (VCaP), 5 μM (LNCaP)[1] |
体外研究
(In Vitro) | ARD-2128 is highly potent and effective in the inhibition of cell growth in the VCaP cell line and LNCaP cell line with the IC50values of 4 nM and 5 nM, respectively[1].
ARD-2128 (1, 10, 100, and 1000 nM; 24 hours) 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, in VCaP cell[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. |
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体内研究
(In Vivo) | 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 Cmax, AUC0-tand t1/2values 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 Cmax, AUC0-tand t1/2were 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(121.90 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.2190 mL | 6.0948 mL | 12.1896 mL | | 5 mM | 0.2438 mL | 1.2190 mL | 2.4379 mL | | 10 mM | 0.1219 mL | 0.6095 mL | 1.2190 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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