| Identification | Back Directory | [Name]
ARCC-4 | [CAS]
1973403-00-7 | [Synonyms]
ARCC-4
ARCC-4 (free base)
(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 | [Molecular Formula]
C53H56F3N7O7S2 | [MDL Number]
MFCD32858266 | [MOL File]
1973403-00-7.mol | [Molecular Weight]
1024.18 |
| Chemical Properties | Back Directory | [density ]
1.39±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 200 mg/mL (195.28 mM) | [form ]
Solid | [pka]
13.63±0.46(Predicted) | [color ]
White to off-white | [Water Solubility ]
Water: < 0.1 mg/mL (insoluble) |
| Hazard Information | Back Directory | [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 | [IC 50]
VHL | [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. |
|
| Company Name: |
csynbio
|
| Tel: |
15051477682 |
| Website: |
m.is0513.com/showsupplierproductslist1949820/0.htm |
|