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Cat. No. M9105
ARV-771 Structure


Size Price Availability Quantity
10mM*1mL In DMSO USD 650 In stock
2mg USD 330 In stock
5mg USD 430 In stock
10mg USD 610 In stock
25mg USD 1180 In stock
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Quality Control
Biological Activity

ARV-771 is a small-molecule pan-BET degrader with Kd values of 4.7, 7.6, 7.6 nM against BRD2, BRD3 and BRD4, respectively. ARV-771 potently degrades BRD2/3/4 in 22Rv1 cells with a DC50 less than 5 nM. c-MYC protein is a downstream effector of BET proteins. Treatment with ARV-771 results in depletion of c-MYC with an IC50 of less than 1 nM. ARV-771 shows strong antiproliferative effect on 22Rv1, VCaP, and LnCaP95 cell lines.

In vivo, treatment of non castrated male Nu/Nu mice bearing AR-V7+ 22Rv1 tumor xenografts with daily subcutaneous injections of ARV-771 at 10 mg/kg for 3 d results in 37% and 76% down-regulation of BRD4 and c-MYC levels, respectively, in tumor tissue.

Cell Experiment
Cell lines 22Rv1 cells
Preparation method ARV-771 is dissolved in DMSO. 22Rv1 cells (5,000 cells per well) are dosed with ARV-771 serially diluted 1:3 for a 10-point dose curve for 72 h. CellTiter-Glo Luminescent Cell Viability Assay is added, and the plate is read on a luminometer. Data are analyzed and plotted using GraphPad Prism software.
Incubation time 72 h
Animal Experiment
Animal models Mice bearing tumors
Dosages (5, 10, 30, 50 mg/kg) for up to 3 wk
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 986.64
Formula C49H60ClN9O7S2
CAS Number 1949837-12-0
Purity >98%
Solubility DMSO 10 mM
Storage at -20°C

Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells.
Saenz DT, et al. Leukemia. 2017 Sep;31(9):1951-1961. PMID: 28042144.

PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer.
Raina K, et al. Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7124-9. PMID: 27274052.

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Abmole Inhibitor Catalog 2017

Keywords: ARV-771, ARV771 supplier, Epigenetic Reader Domain, inhibitors

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