Free shipping on all orders over $ 500

ARV-771

Cat. No. M9105
ARV-771 Structure
Synonym:

ARV771

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
Free Delivery on orders over USD 500 Bulk Inquiry?

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.

Protocol
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.
Concentrations
Incubation time 72 h
Animal Experiment
Animal models Mice bearing tumors
Formulation
Dosages (5, 10, 30, 50 mg/kg) for up to 3 wk
Administration
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
References

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.

Related Epigenetic Reader Domain Products
AZD5153

AZD5153 is a potent bivalent triazolopyridazine based Bromodomain and Extraterminal (BET) Inhibitor, with IC50 value of 5 nM.

MS417

MS417 (also known as GTPL7512) is a potent and selective BRD4 inhibitor, which binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30 and 46 nM, respectively.

FL-411

FL-411 is a selective BRD4 inhibitor.

dBET6

dBET6 is a highly potent, selective and cell-permeable degrader of BET with an IC50 of 14 nM.

dBET1

dBET1 is a potent BRD4 protein degrader with an EC50 of 430 nM.

  Catalog
Abmole Inhibitor Catalog 2017




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

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.