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ARCC-4

Catalog No. T14318   CAS 1973403-00-7

ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide and it is a low-nanomolar androgen receptor (AR) degrader based on PROTAC, with a DC50 of 5 nM. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy[1].

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ARCC-4 Chemical Structure
ARCC-4, CAS 1973403-00-7
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Biological Description
Chemical Properties
Storage & Solubility Information
Description ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide and it is a low-nanomolar androgen receptor (AR) degrader based on PROTAC, with a DC50 of 5 nM. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy[1].
In vitro ARCC-4 selectively degrades AR via the proteasome but not PR-A or PR-B suppression[1] and it shows efficacy against clinically relevant AR mutations[1]. ARCC-4 maintains activity despite elevated androgen levels[1]. ARCC-4 enhances protein-protein interactions between AR and VHL, thereby promoting the association of the trimeric complex[1] and it induces apoptosis and inhibiting proliferation of AR-amplified prostate cancer cells[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].
Molecular Weight 1024.18
Formula C53H56F3N7O7S2
CAS No. 1973403-00-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

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.

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Keywords

ARCC-4 1973403-00-7 Others ARCC 4 ARCC4 inhibitor inhibit

 

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