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Submit ReviewARV 771
Description: Potent BET bromodomain PROTAC®; also degrades BRD-tagged chimeric antigen receptors (CAR) in T cells
Chemical Name: (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
Purity: ≥98% (HPLC)
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. 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.
Technical Data for ARV 771
| M. Wt | 986.65 |
| Formula | C49H60ClN9O7S2 |
| Storage | Store at -20°C |
| Purity | ≥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 |
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 | |
|---|---|---|---|
| Solubility | |||
| DMSO | 98.67 | 100 |
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 |
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Product Datasheets for ARV 771
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, Bromodomain, (BRD), 7256, Tocris Bioscience
Citations for ARV 771
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TPD and Induced Proximity Research Product GuideUpdated
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
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