Catalog No. size PriceQuantity
M7147-2 2 mg solid $300
M7147-10 10 mg solid $1,065
M7147-C Contact for quotation $100


ARCC 4 is a PROTAC, acting as an androgen receptor degrader. ARCC-4 is a low-nanomolar androgen receptor degrader able to degrade about 95% of cellular androgen receptors. ARCC-4 inhibits prostate tumor cell proliferation, degrades clinically relevant androgen receptor point mutants and unlike enzalutamide, retains antiproliferative effect in a high androgen environment. Thus, ARCC-4 exemplifies how protein degradation can address the drug resistance hurdles of enzalutamide.

Product information

CAS Number: 1973403-00-7

Molecular Weight: 1024.18

Formula: C53H56F3N7O7S2




ARCC-4 hydrate


Related CAS Number:

1973403-00-7 (free base)

Chemical Name: (2S,4R)-1-[(2S)-2-(2-[4-[4-(4-[3-[4-Cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-sulfanylideneimidazolidin-1-yl]phenyl)phenoxy]butoxy]acetamido)-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide

Smiles: CC(C)(C)[C@H](NC(=O)COCCCCOC1C=CC(=CC=1)C1C=CC(=CC=1)N1C(=S)N(C(=O)C1(C)C)C1=CC(=C(C=C1)C#N)C(F)(F)F)C(=O)N1C[C@H](O)C[C@H]1C(=O)NCC1C=CC(=CC=1)C1SC=NC=1C


InChi: InChI=1S/C53H56F3N7O7S2/c1-32-45(72-31-59-32)36-11-9-33(10-12-36)28-58-47(66)43-26-40(64)29-61(43)48(67)46(51(2,3)4)60-44(65)30-69-23-7-8-24-70-41-21-16-35(17-22-41)34-13-18-38(19-14-34)63-50(71)62(49(68)52(63,5)6)39-20-15-37(27-57)42(25-39)53(54,55)56/h9-22,25,31,40,43,46,64H,7-8,23-24,26,28-30H2,1-6H3,(H,58,66)(H,60,65)/t40-,43+,46-/m1/s1

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

ARCC-4 induces apoptosis and inhibiting proliferation of AR-amplified prostate cancer cells. ARCC-4 enhances protein-protein interactions between AR and VHL, thereby promoting the association of the trimeric complex. ARCC-4 (0.1-10, 000 nM; 20 hours) potently degrades AR with a D50 of 5 nM and Dmax of over 95%. ARCC-4 (100 nM; 12 hours) shows near complete AR degradation (>98%) in prostate cancer cells. ARCC-4 selectively degrades AR via the proteasome but not PR-A or PR-B suppression. ARCC-4 shows efficacy against clinically relevant AR mutations. ARCC-4 maintains activity despite elevated androgen levels.


  1. Salami J, Alabi S, Willard RR, Vitale NJ, Wang J, Dong H, Jin M, McDonnell DP, Crew AP, Neklesa TK, Crews CM. 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. doi: 10.1038/s42003-018-0105-8. eCollection 2018. PubMed PMID: 30271980; PubMed Central PMCID: PMC6123676.

Products are for research use only. Not for human use.

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