ARV 771

Name: ARV 771
Brand: Tocris Bioscience
SKU: 7256

Tocris Bioscience, part of Bio-Techne | Catalog # 7256

Citations (1)

COA / SDS

Potent BET bromodomain PROTAC®; also degrades BRD-tagged chimeric antigen receptors (CAR) in T cells

Key Product Details

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)
Molecular Weight:	986.65

View Full Technical Details for ARV 771

Technical Data
Citations

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 for ARV 771

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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	0.20 mL	1.01 mL	2.03 mL
10 mM	0.10 mL	0.51 mL	1.01 mL
50 mM	0.02 mL	0.10 mL	0.20 mL

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References for ARV 771

References are publications that support the biological activity of the product.

Saenz Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells. Leukemia 2017 PMID: 28042144
Lee A chemical switch system to modulate chimeric antigen receptor T cell activity through proteolysis-targeting chimaera technology. ACS Synth.Biol. 2020 PMID: 32352759
Raina PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proc.Natl.Acad.Sci.U.S.A. 2016 PMID: 27274052