1973403-00-7
1973403-00-7 structure
- Name: ARCC 4
- Chemical Name: ARCC-4
- CAS Number: 1973403-00-7
- Molecular Formula: C53H56F3N7O7S2
- Molecular Weight: 1024.18
- Catalog: Signaling Pathways PROTAC PROTAC
- Create Date: 2020-06-01 11:02:36
- Modify Date: 2024-01-16 10:35:36
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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].
| Name | ARCC-4 |
|---|
| Description | 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]. |
|---|---|
| Related Catalog | |
| Target |
VHL |
| In Vitro | 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 Concentration: 0.1 nM, 1 nM, 10 nM, 50 nM, 100 nM, 0.5μM, 1μM, 10 μM Incubation Time: 20 hours Result: Potently degrades AR |
| References |
| Molecular Formula | C53H56F3N7O7S2 |
|---|---|
| Molecular Weight | 1024.18 |
| Hazard Codes | Xi |
|---|