ARD-2128
- CAS No.
- 2222111-87-5
- Chemical 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]-
- CBNumber:
- CB79731270
- Molecular Formula:
- C45H50ClN7O6
- Molecular Weight:
- 820.37
- MDL Number:
- MFCD34567333
- MOL File:
- 2222111-87-5.mol
ARD-2128 Chemical Properties,Uses,Production
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].
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
Raw materials
Preparation Products
ARD-2128 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 | sales-cpd@caerulumpharma.com | China | 3431 | 58 |
| DC Chemicals | 021-58447131 13564518121 | sales@dcchemicals.com | China | 9412 | 58 |
| Chunchuang (Wuhan) Technology Co., Ltd | 15342225168 | yutianchun2007@126.com | China | 10009 | 58 |
| Changzhou Borl Biotechnology Co.,LTD | 13606124132;13656121842 | luyan0021@163.com | China | 217 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24017 | 58 |
| Nantong QuanYi Biotechnology Co., Ltd | 0513-66337626 18051384581 | sales@chemhifuture.com | China | 4371 | 58 |
| Shanghai Easy CDMO Co.,Ltd | 021-61734564 | August@easycdmo.com | China | 10010 | 58 |
| Suzhou Haiben Pharmaceutical Co., Ltd | 14760821013 14760821013 | 1816280386@qq.com | China | 5208 | 58 |