ARV-771 ( ARV 771;ARV771 )

Catalog No. M13050 CAS No. 1949837-12-0

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

ARV-771
Note

Research use only, not for human use.
Brief Description

ARV-771 is a potent BET degrader (PROTAC) in cellular models of CRPC; potently degrades BRD2/3/4 in 22Rv1 cells with DC50< 5 nM.
Description

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

ARV 771;ARV771
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

Bromodomain
Research Area

——
Indication

——

CAS Number

1949837-12-0
Formula Weight

986.64
Molecular Formula

C49H60ClN9O7S2
Purity

>98% (HPLC)
Solubility

10 mM in DMSO
SMILES

CC1=C(C)C(C(C2=CC=C(C)C=C2)=N[C@H]3CC(NCCOCCCOCC(N[C@@H](C(C)(C)C)C(N4[C@H](C(N[C@@H](C)C5=CC=C(C6=C(C)N=CS6)C=C5)=O)C[C@@H](O)C4)=O)=O)=O)=C(S1)N7C3=NN=C7C
Chemical Name

(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

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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