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Biological Activity 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.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Technical Data for ARV 771
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for ARV 771
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for ARV 771
The following data is based on the product molecular weight 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.
|Concentration / Solvent Volume / Mass||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|
References for ARV 771
References are publications that support the biological activity of the product.
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.
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Keywords: ARV 771, ARV 771 supplier, ARV771, PROTACs, Degraders, degrades, potent, BET, bromodomains, BRD4, VHL, von, Hippel, Lindau, chimeric, antigen, receptors, CAR-T, cells, Bromodomains, Active, 7256, Tocris Bioscience
Citations for ARV 771
Citations are publications that use Tocris products.
Currently there are no citations for ARV 771. Do you know of a great paper that uses ARV 771 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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Epigenetics Scientific Review
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Epigenetics in Cancer Poster
Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
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