| Chemical Properties | Back Directory | [Boiling point ]
1000.4±65.0 °C(Predicted) | [density ]
1.39±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Acetonitrile: Slightly Soluble: 1-10 mg/ml | [form ]
Solid | [pka]
10.83±0.40(Predicted) | [color ]
Light yellow to green yellow |
| Hazard Information | Back Directory | [Uses]
ARD-2128 is a highly potent, orally bioavailable PROTAC androgen 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 prostate cancer[1]. | [Biological Activity]
ARD-2128 is a highly potent, orally bioavailable PROTAC androgen 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 prostate cancer[1].
ARD-2128 is highly potent and effective in the inhibition of cell growth in the VCaP cell line and LNCaP cell line with the IC50 values 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].
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-t and t1/2 values of 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively[1]. | [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-t and t1/2 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 Cmax, AUC0-t and t1/2 were 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively.
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| [References]
[1]. Han X, et al. Strategies toward Discovery of Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer [published online ahead of print, 2021 Aug 25]. J Med Chem. 2021;10.1021/acs.jmedchem.1c00882. |
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