ARV 771

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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)
Literature (4)

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

M. Wt 986.65
Formula C49H60ClN9O7S2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1949837-12-0
PubChem ID 126619980
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
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.

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 0.2 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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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.

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

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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

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