|N-(反式-4-(3-氯-4-氰基苯氧基)环己基)-6-(4-((4-(2-(2,6-二氧代哌啶-3-基)-6-氟-1,3-二氧代异吲哚啉-5-基)哌嗪-1-基)甲基)哌啶-1-基)哒嗪-3-甲酰胺|CsnPharm

CAS No.: 2222112-77-6

N-(trans-4-(3-Chloro-4-cyanophenoxy)cyclohexyl)-6-(4-((4-(2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxoisoindolin-5-yl)piperazin-1-yl)methyl)piperidin-1-yl)pyridazine-3-carboxamide Catalog No. CSN28405

Synonyms: ARV-110

ARV-110 is an orally active, specific androgen receptor PROTAC degrader with DC50 < 1nM.

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400-920-2911

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生物活性

描述Protease-targeted chimeras (PROTACs) molecules are bifunctional small molecules that simultaneously bind a target protein and an E3-ubiquitin ligase, thus causing ubiquitination and degradation of the target protein by the proteasome. Like small molecules, PROTAC molecules possess good tissue distribution and the ability to target intracellular proteins^[2]. ARV-110, an orally small molecule PROTAC was designed to specifically target Androgen receptor (AR), firstly enters clinical phase I trials for the treatment of metastatic castration-resistant prostate cancer, which turns a new avenue for the development of PROTAC^[3]. ARV-110 robustly degrades AR in all cell lines tested, with an observed halfmaximal degradation concentration (DC50) of ~1 nM. ARV-110 treatment leads to highly selective AR degradation, as demonstrated by proteomic studies. In VCaP cells,PROTAC-mediated AR degradation suppresses the expression of the AR-target gene PSA, inhibits AR-dependent cell proliferation, and induces apoptosis at low nanomolar concentrations. Further, ARV-110 degrades clinically relevant mutant AR proteins and retains activity in a high androgen environment. In mouse xenograft studies, greater than 90% AR degradation is observed at a 1 mg/kg PO QD dose. Notably, ARV-110 demonstrates in vivo efficacy and reduction of AR-target gene expression in a long term, castrate,enzalutamide-resistant VCaP tumor modelz^[4]. Clinical activity for ARV-110 in heavily pretreated patients with mCRPC and suggested enhanced activity in patients with specific molecular profiles, eg, AR T878 and H875 mutations (ARV-110 doses ranged from 35–700 mg QD or 210–420 mg BID)^[5].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.2311 mL
- 6.1555 mL
- 12.3109 mL
- 5 mM
- 0.2462 mL
- 1.2311 mL
- 2.4622 mL
- 10 mM
- 0.1231 mL
- 0.6155 mL
- 1.2311 mL

技术信息

CAS号	2222112-77-6	储存条件	粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C41H43ClFN9O6	运输	蓝冰
分子量	812.29	别名	ARV-110

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N-(trans-4-(3-Chloro-4-cyanophenoxy)cyclohexyl)-6-(4-((4-(2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxoisoindolin-5-yl)piperazin-1-yl)methyl)piperidin-1-yl)pyridazine-3-carboxamide Catalog No. CSN28405

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