A PROTAC that drives BET family protein degradation; induces degradation of BRD2

ARV-771 – 5 mg

Brand:
Cayman
CAS:
1949837-12-0
Storage:
-20
UN-No:
Non-Hazardous - /

ARV-771 is a proteolysis-targeting chimera (PROTAC) that drives the degradation of bromodomain and extra terminal domain (BET) family proteins.{33349} It is comprised of a BET-binding moiety conjugated via a linker to a von Hippel-Lindau (VHL) E3 ligase-binding moiety. ARV-771 induces degradation of bromodomain-containing protein 2 (BRD2), BRD3, and BRD4 in 22Rv1 castration-resistant prostate cancer (CRPC) cells with half-maximal degradation (DC50) values of less than 5 nM for all. It inhibits proliferation of and increases poly(ADP-ribose) polymerase (PARP) cleavage in 22Rv1 cells in a concentration-dependent manner. ARV-771 reduces full-length androgen receptor protein levels and prevents increases in ERG induced by the synthetic androgen R1881 in VCaP cells in a concentration-dependent manner. ARV-771 (30 mg/kg per day, s.c.) induces tumor regression in a 22Rv1 mouse xenograft model.  

 

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Description

A PROTAC that drives BET family protein degradation; induces degradation of BRD2, BRD3, and BRD4 in 22Rv1 CRPC cells (DC50s = <5 nM for all); inhibits proliferation of and increases PARP cleavage in 22Rv1 cells in a concentration-dependent manner; reduces full-length androgen receptor protein levels and prevents R1881-induced increases in ERG in VCaP cells; induces tumor regression in a 22Rv1 mouse xenograft model at 30 mg/kg per day, s.c.

Formal 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

Synonyms: 

Molecular weight: 986.6

CAS: 1949837-12-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|PROTACs||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Androgens||Research Area|Epigenetics, Transcription, & Translation|Readers|Bromodomains

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