ARV-771 - 98%, high purity , CAS No.1949837-12-0, Inhibitor of bromodomain containing 2;Inhibitor of bromodomain containing 3;Inhibitor of bromodomain containing 4

Item Number

A414042

• Specifications & Purity: Moligand™, ≥98%
• Biochemical and Physiological Mechanisms: ARV-771 is a potent pan-(bromodomain and extra-terminal)BET degrader, a novel BET-PROTAC(proteolysis-targeting chimera) with Kd of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Inhibitor of bromodomain containing 2;Inhibitor of bromodomain containing 3;Inhibitor of bromodomain containing 4

Product Description

Information

ARV-771 is a potent pan-(bromodomain and extra-terminal)BET degrader, a novel BET-PROTAC(proteolysis-targeting chimera) with Kd of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively.

Targets

BRD2-BD2 (Cell-free assay); BRD3-BD2 (Cell-free assay); BRD4-BD2 (Cell-free assay); BRD3-BD1 (Cell-free assay); BRD4-BD1 (Cell-free assay) 32850,4.7 nM(Kd); 7.6 nM(Kd); 7.6 nM(Kd); 8.3 nM(Kd); 9.6 nM(Kd)

In vitro

ARV-771 is a potent small-molecule pan-BET degrader based on proteolysis-targeting chimera (PROTAC) technology, demonstrates dramatically improved efficacy in cellular models of CRPC as compared with BET inhibition. ARV-771 treatment of CRPC cells results in apoptosis.

In vivo

ARV-771 induces degradation in vivo. ARV-771 results in suppression of both AR signaling and AR levels and leads to tumor regression in a CRPC mouse xenograft model.

Cell Research(from reference)

Cell lines：22Rv1 cells, VCaP cells, LnCaP95 cells 

Concentrations：1-300 nM 

Incubation Time：24 h, 72 h