ARV 771

Tocris Bioscience | Catalog # 7256

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

Key Product Details

Description

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

Product Description

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.

Product Specifications for ARV 771

Molecular Weight

986.65

Formula

C49H60ClN9O7S2

Storage

Store at -20°C

Purity

≥98% (HPLC)

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

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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Product Documents for ARV 771

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for ARV 771

For research use only

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