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ARV 771

Cat. No. 7256 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent BET bromodomain PROTAC®; also degrades BRD-tagged chimeric antigen receptors (CAR) in T cells
化学名： (2S,4R)-1-((S)-2-(tert-Butyl)-15-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,14-dioxo-6,10-dioxa-3,13-diazapentadecanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide
纯度： ≥98% (HPLC)
说明书
引用文献
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文献 (2)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for ARV 771

ARV 771 is a potent BET bromodomain PROTAC® Degrader (DC50 = < 1nM). Comprises a BRD4-binding moiety joined by a linker to a ligand for Von Hippel-Lindau (VHL) protein. Degrades BRD2/3/4 in castration-resistant prostate cancer (CRPC) cell lines. Reduces androgen receptor levels and induces apoptosis in CRPC cells in vitro. Down-regulates BRD4 and induces tumor regression in CRPC xenografts in mice. Also reduces leukemia burden in a mouse model. Induces degradation of BRD-tagged CAR (chimeric antigen receptor) in T cells. BRD4 antibody validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # NBP1-86640.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

技术数据 for ARV 771

分子量 986.65
公式 C49H60ClN9O7S2
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 1949837-12-0
PubChem ID 126619980
InChI Key PQOGZKGXGLHDGS-QQRWPDCKSA-N
Smiles C[C@@H](C1=CC=C(C2=C(N=CS2)C)C=C1)NC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(COCCCOCCNC(C[C@@H]4N=C(C5=CC=C(C=C5)Cl)C6=C(N7C(C)=NN=C47)SC(C)=C6C)=O)=O)=O)O)=O

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for ARV 771

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 98.67 100

制备储备液 for ARV 771

以下数据基于产品分子量 986.65。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 1.01 mL 5.07 mL 10.14 mL
5 mM 0.2 mL 1.01 mL 2.03 mL
10 mM 0.1 mL 0.51 mL 1.01 mL
50 mM 0.02 mL 0.1 mL 0.2 mL

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参考文献 for ARV 771

参考文献是支持产品生物活性的出版物。

Raina et al (2016) PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proc.Natl.Acad.Sci.U.S.A. 113 7124 PMID: 27274052

Saenz et al (2017) Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells. Leukemia 31 1951 PMID: 28042144

Lee et al (2020) A chemical switch system to modulate chimeric antigen receptor T cell activity through proteolysis-targeting chimaera technology. ACS Synth.Biol. 9 987 PMID: 32352759

If you know of a relevant reference for ARV 771, please let us know.

按标靶查看相关产品

关键词: ARV 771, ARV 771 supplier, ARV771, PROTACs, Degraders, degrades, potent, BET, bromodomains, BRD4, VHL, von, Hippel, Lindau, chimeric, antigen, receptors, CAR-T, cells, Bromodomains, Bromodomain, (BRD), 7256, Tocris Bioscience

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该领域的文献

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TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia