ARCC-4

Product Name: ARCC-4
CAS No.: 1973403-00-7
Chemical Name: ARCC-4
Synonyms: ARCC-4;ARCC-4 (free base);L-Prolinamide, N-[2-[4-[[4'-[3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl][1,1'-biphenyl]-4-yl]oxy]butoxy]acetyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-;(2S,4R)-1-((S)-2-(2-(4-((4'-(3-(4-Cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-[1,1'-biphenyl]-4-yl)oxy)butoxy)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide;(4R)?-N-?[2-?[4-?[[4'-?[3-?[4-?Cyano-?3-?(trifluoromethyl)?phenyl]?-?5,?5-?dimethyl-?4-?oxo-?2-?thioxo-?1-?imidazolidinyl]?[1,?1'-?biphenyl]?-?4-?yl]?oxy]?butoxy]?acetyl]?-?3-?methyl-?L-?valyl-?4-?hydroxy-?N-?[[4-?(4-?methyl-?5-?thiazolyl)?phenyl]?methyl]?-?(L)-?prolinamide
CBNumber: CB68054616
Molecular Formula: C53H56F3N7O7S2
Formula Weight: 1024.18
MOL File: 1973403-00-7.mol

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ARCC-4 Property

Density: 1.39±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO: 200 mg/mL (195.28 mM)
pka: 13.63±0.46(Predicted)
form: Solid
color: White to off-white
Water Solubility: Water: < 0.1 mg/mL (insoluble)

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Tocris

Product number: 7254
Product name: ARCC4
Purity: ≥98%(HPLC)
Packaging: 5
Price: $369
Updated: 2021/12/16

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ARCC-4 Chemical Properties,Usage,Production

Uses

(4R)??-N-??[2-??[4-??[[4'-??[3-??[4-??Cyano-??3-??(trifluoromethyl)??phenyl]??-??5,??5-??dimethyl-??4-??oxo-??2-??thioxo-??1-??imidazolidinyl]??[1,??1'-??biphenyl]??-??4-??yl]??oxy]??butoxy]??acetyl]??-??3-??methyl-??L-??valyl-??4-??hydroxy-??N-??[[4-??(4-??methyl-??5-??thiazolyl)??phenyl]??methyl]??-??(L)-??prolinamide is required for the targeted degradation of the androgen receptor.

Biological Activity

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]. 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

storage

Store at -20°C

References

[1]. Salami J, et al. 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.

ARCC-4 Preparation Products And Raw materials

Raw materials

Preparation Products

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ARCC-4 Suppliers

China 13 United States 3 Global 16

ShangHai Caerulum Pharma Discovery Co., Ltd.

Tel: 18149758185 18149758185
Email: sales-cpd@caerulumpharma.com
Country: China
ProdList: 3466
Advantage: 58

Sichuan Wei Keqi Biological Technology Co., Ltd.

Tel: 028-81700200 18116577057
Fax: 028-81705658
Email: 3003855609@qq.com
Country: China
ProdList: 7887
Advantage: 56

Jilin Province Woda Biotechnology Co., Ltd.

Tel: 13504435624
Email: 1927928688@qq.com
Country: China
ProdList: 1388
Advantage: 58

TargetMol Chemicals Inc.

Tel: +1-781-999-5354 +1-00000000000
Email: marketing@targetmol.com
Country: United States
ProdList: 32080
Advantage: 58

csynbio

Tel: 15051477682
Email: changming.pan@csynbio.com
Country: China
ProdList: 243
Advantage: 58

Bide Pharmatech Ltd.

Tel: 400-1647117 13681763483
Email: product02@bidepharm.com
Country: China
ProdList: 62163
Advantage: 58

Changzhou Bojia Biomedical Technology Co., Ltd.

Tel: 2122619822
Email: czbjpharma@126.com
Country: China
ProdList: 18478
Advantage: 58

TargetMol Chemicals Inc.

Tel: 4008200310
Email: marketing@tsbiochem.com
Country: China
ProdList: 24647
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ShenZhen Trendseen Biological Technology Co.,Ltd.

Tel: 13417589054 13417589054
Email: trendseenbio@gmail.com
Country: China
ProdList: 9470
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Nantong QuanYi Biotechnology Co., Ltd

Tel: 0513-66337626 18051384581
Email: sales@chemhifuture.com
Country: China
ProdList: 4870
Advantage: 58

1973403-00-7, ARCC-4Related Search:

3-Pyridazinecarboxamide, N-[trans-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-[[4-[2-(2,6-dioxo-3-piperidinyl)-6-fluoro-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]-1-piperazinyl]methyl]-1-piperidinyl]- ARV-771 ARV-825 ARV-471

ARCC-4

(4R)?-N-?[2-?[4-?[[4'-?[3-?[4-?Cyano-?3-?(trifluoromethyl)?phenyl]?-?5,?5-?dimethyl-?4-?oxo-?2-?thioxo-?1-?imidazolidinyl]?[1,?1'-?biphenyl]?-?4-?yl]?oxy]?butoxy]?acetyl]?-?3-?methyl-?L-?valyl-?4-?hydroxy-?N-?[[4-?(4-?methyl-?5-?thiazolyl)?phenyl]?methyl]?-?(L)-?prolinamide

ARCC-4 (free base)

L-Prolinamide, N-[2-[4-[[4'-[3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl][1,1'-biphenyl]-4-yl]oxy]butoxy]acetyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-

(2S,4R)-1-((S)-2-(2-(4-((4'-(3-(4-Cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-[1,1'-biphenyl]-4-yl)oxy)butoxy)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

1973403-00-7