ARCC-4
- Product Name
- 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)-;(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
- Formula Weight
- 1024.18
- MOL File
- 1973403-00-7.mol
ARCC-4 Property
- Density
- 1.39±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: 200 mg/mL (195.28 mM)
- pka
- 13.63±0.46(Predicted)
- Water Solubility
- Water: < 0.1 mg/mL (insoluble)
N-Bromosuccinimide Price
- Product number
- 7254
- Product name
- ARCC4
- Purity
- ≥98%(HPLC)
- Packaging
- 5
- Price
- $369
- Updated
- 2021/12/16
ARCC-4 Chemical Properties,Usage,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
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