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| | ARD-2128 Basic information |
| Product Name: | ARD-2128 | | Synonyms: | ARD-2128;orally,ARD2128,AR-regulated,bioavailable,inhibit,ARD 2128,Inhibitor,prostate,Androgen Receptor,cancer,ARD-2128,tumor,PROTACs;Benzamide, N-[trans-3-(3-chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]-4-[4-[[1-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]-4-piperidinyl]methyl]-1-piperazinyl]-;N-[trans-3-(3-Chloro-4-cyanophenoxy)-2,2,4,4-tetramethylcyclobutyl]-4-[4-[[1-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]-4-piperidinyl]methyl]-1-piperazinyl]benzamide | | CAS: | 2222111-87-5 | | MF: | C45H50ClN7O6 | | MW: | 820.37 | | EINECS: | | | Product Categories: | | | Mol File: | 2222111-87-5.mol |  |
| | ARD-2128 Chemical Properties |
| 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 |
| | ARD-2128 Usage And Synthesis |
| 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. |
| | ARD-2128 Preparation Products And Raw materials |
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