[CAS NO. 1973403-00-7] ARCC-4
PRODUCTS SPECIFICATIONS [1973403-00-7]
DESCRIPTION [1973403-00-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 1024.18 |
| Molecular Formula | C53H56F3N7O7S2 |
| SMILES | O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@H]3N(C([C@H](C(C)(C)C)NC(COCCCCOC4=CC=C(C5=CC=C(N(C(N6C7=CC=C(C#N)C(C(F)(F)F)=C7)=S)C(C)(C)C6=O)C=C5)C=C4)=O)=O)C[C@H](O)C3 |
Summary
ARCC-4 is a low-nanomolar Androgen Receptor (AR) degrader based on PROTAC , with a DC 50 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] .
IC50 & 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 D
50
of 5 nM and D
max
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 200 mg/mL ( 195.28 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 0.9764 mL | 4.8820 mL | 9.7639 mL |
| 5 mM | 0.1953 mL | 0.9764 mL | 1.9528 mL |
| 10 mM | 0.0976 mL | 0.4882 mL | 0.9764 mL |