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ARCC-4 

Cat. No.: HY-130492 Purity: 99.22%
Handling Instructions

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.

For research use only. We do not sell to patients.

ARCC-4 Chemical Structure

ARCC-4 Chemical Structure

CAS No. : 1973403-00-7

Size Price Stock Quantity
1 mg USD 550 In-stock
Estimated Time of Arrival: December 31
5 mg USD 1250 In-stock
Estimated Time of Arrival: December 31
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50 mg   Get quote  

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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].

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 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].

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
Molecular Weight

1024.18

Formula

C₅₃H₅₆F₃N₇O₇S₂

CAS No.

1973403-00-7

SMILES

O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[[email protected]]3N(C([[email protected]](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[[email protected]](O)C3

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
In Vitro: 

DMSO : 200 mg/mL (195.28 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 5 mg/mL (4.88 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 5 mg/mL (4.88 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (4.88 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

ARCC-4ARCC4ARCC 4PROTACAndrogen ReceptorProteolysis-targeting chimeraInhibitorinhibitorinhibit

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ARCC-4
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HY-130492
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