ARCC-4

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vonHippel-Lindau(VHL)招募的ARPROTAC。ARCC-4能有效降解与抗雄激素研究相关的AR突变。

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库存: 现货

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5mg

￥4100.00

3280.00

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10mg

￥6475.00

5180.00

- +
25mg

￥12287.00

9830.00

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货号: ajcx30182
CAS: 1973403-00-7
别名:
分子式: C53H56F3N7O7S2
分子量: 1024.18
纯度: >98%
溶解度: DMSO: 200 mg/mL (195.28 mM); Water: < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

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

[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.