ARCC-4
- CAS No.
- 1973403-00-7
- Chemical Name:
- ARCC-4
- Synonyms
- ARCC-4;ARCC-4 (free base);L-Prolinamide, N-[2-[4-[[4'-[3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl][1,1'-biphenyl]-4-yl]oxy]butoxy]acetyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-;(2S,4R)-1-((S)-2-(2-(4-((4'-(3-(4-Cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-[1,1'-biphenyl]-4-yl)oxy)butoxy)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide;(4R)?-N-?[2-?[4-?[[4'-?[3-?[4-?Cyano-?3-?(trifluoromethyl)?phenyl]?-?5,?5-?dimethyl-?4-?oxo-?2-?thioxo-?1-?imidazolidinyl]?[1,?1'-?biphenyl]?-?4-?yl]?oxy]?butoxy]?acetyl]?-?3-?methyl-?L-?valyl-?4-?hydroxy-?N-?[[4-?(4-?methyl-?5-?thiazolyl)?phenyl]?methyl]?-?(L)-?prolinamide
- CBNumber:
- CB68054616
- Molecular Formula:
- C53H56F3N7O7S2
- Molecular Weight:
- 1024.18
- MDL Number:
- MFCD32858266
- MOL File:
- 1973403-00-7.mol
ARCC-4 Chemical Properties,Uses,Production
Uses
(4R)??-N-??[2-??[4-??[[4'-??[3-??[4-??Cyano-??3-??(trifluoromethyl)??phenyl]??-??5,??5-??dimethyl-??4-??oxo-??2-??thioxo-??1-??imidazolidinyl]??[1,??1'-??biphenyl]??-??4-??yl]??oxy]??butoxy]??acetyl]??-??3-??methyl-??L-??valyl-??4-??hydroxy-??N-??[[4-??(4-??methyl-??5-??thiazolyl)??phenyl]??methyl]??-??(L)-??prolinamide is required for the targeted degradation of the androgen receptor.
Biological Activity
ARCC-4 is a low-nanomolar androgen receptor (AR) degrader based on PROTAC, with a DC50 of 5 nM. ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy[1]. ARCC-4 induces apoptosis and inhibiting proliferation of AR-amplified prostate cancer cells[1].ARCC-4 enhances protein-protein interactions between AR and VHL, thereby promoting the association of the trimeric complex[1].ARCC-4 (0.1-10,000 nM; 20 hours) potently degrades AR with a D50 of 5 nM and Dmax of over 95%[1].ARCC-4 (100 nM; 12 hours) shows near complete AR degradation (>98%) in prostate cancer cells[1]. ARCC-4 selectively degrades AR via the proteasome but not PR-A or PR-B suppression[1].ARCC-4 shows efficacy against clinically relevant AR mutations[1].ARCC-4 maintains activity despite elevated androgen levels[1]. Western Blot Analysis[1] Cell Line: VCaP cells
storage
Store at -20°C
References
[1]. Salami J, et al. Androgen receptor degradation by the proteolysis-targeting chimera ARCC-4 outperforms enzalutamide in cellular models of prostate cancer drug resistance. Commun Biol. 2018 Aug 2;1:100.
ARCC-4 Preparation Products And Raw materials
Raw materials
Preparation Products
ARCC-4 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 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 | 3466 | 58 |
Sichuan Wei Keqi Biological Technology Co., Ltd. | 028-81700200 18116577057 | 3003855609@qq.com | China | 7887 | 56 |
Shanghai Chaolan Chemical Technology Center | QQ:65489617 15618227136 | info@SuperLan-chem.com | China | 9943 | 58 |
Jilin Province Woda Biotechnology Co., Ltd. | 13504435624 | 1927928688@qq.com | China | 1382 | 58 |
csynbio | 15051477682 | changming.pan@csynbio.com | China | 242 | 58 |
Bide Pharmatech Ltd. | 400-1647117 13681763483 | product02@bidepharm.com | China | 62163 | 58 |
Changzhou Bojia Biomedical Technology Co., Ltd. | 2122619822 | czbjpharma@126.com | China | 18488 | 58 |
ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 13417589054 | trendseenbio@gmail.com | China | 9880 | 58 |