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  3. ARCC-4

ARCC-4 

目录号: HY-130492
产品使用指南

ARCC-4 是基于 PROTAC 技术的,纳摩尔级的雄激素受体 (AR) 降解剂,其 D50 值为 5 nM。ARCC-4 是一种基于 enzalutamide 的 von Hippel-Lindau (VHL) 招募的 AR PROTAC。ARCC-4 能有效降解与抗雄激素研究相关的 AR 突变。

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ARCC-4 Chemical Structure

ARCC-4 Chemical Structure

CAS No. : 1973403-00-7

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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].

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)[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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

  • 稀释计算器

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× = ×
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Keywords:

ARCC-4ARCC4ARCC 4PROTACAndrogen ReceptorProteolysis-targeting chimeraInhibitorinhibitorinhibit

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ARCC-4
目录号:
HY-130492
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