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ARV-771

Chemical Structure : ARV-771

CAS No.: 1949837-12-0

ARV-771 (ARV 771;ARV771)

Catalog No.: PC-42297Not For Human Use, Lab Use Only.

ARV-771 is a potent BET degrader (PROTAC), potently degrades BRD2/3/4 in 22Rv1 cells with DC50< 5 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

ARV-771 is a potent BET degrader (PROTAC), potently degrades BRD2/3/4 in 22Rv1 cells with DC50< 5 nM.
ARV-771 is equally potent activity in VCaP and LnCaP95 CRPC cell lines, causes depletion of c-MYC with IC50<1 nM.
ARV-771 suppresses both AR signaling and AR levels and leads to tumor regression in a CRPC mouse xenograft model.

Physicochemical Properties

M.Wt 986.6398
Formula C49H60ClN9O7S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2S,4R)-1-((2S)-2-(tert-butyl)-15-((6S)-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-diazapentadecan-1-oyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-c

References

1. Raina K, et al. Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7124-9.

2. Saenz DT, et al. Leukemia. 2017 Jan 31. doi: 10.1038/leu.2016.393.

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