SML3423
ARV-825
≥98% (HPLC)
Synonym(s):
(6S)-4-(4-chlorophenyl)-N-[4-[2-[2-[2-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]ethoxy]ethoxy]ethoxy]phenyl]-2,3,9-trimethyl-6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide
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About This Item
Empirical Formula (Hill Notation):
C46H47ClN8O9S
CAS Number:
Molecular Weight:
923.43
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality Segment
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
SMILES string
ClC1=CC=C(C2=N[C@@H](CC(NC3=CC=C(C=C3)OCCOCCOCCOCCNC4=C(C5=CC=C4)C(N(C5=O)C6C(NC(CC6)=O)=O)=O)=O)C7=NN=C(C)N7C8=C2C(C)=C(C)S8)C=C1
InChI key
RWLOGRLTDKDANT-TYIYNAFKSA-N
Biochem/physiol Actions
ARV-825 is a hetero-bifunctional PROteolysis TArgeting Chimera (PROTAC) containing a BRD4 binding group (OTX-015) on one end, a linker arm, and a cereblon (CRBN) ubiquitin E3 ligase binding group (Pomalidomide) on the other end, resulting in BRD4 ubiquitylation and degradation by the proteasome. In Burkitt’s lymphoma cells, ARV-825 was found to cause prolonged BRD4 downregulation, reduce c-Myc levels, block cell proliferation, and induce apoptosis with improved results compared to BRD4 inihbitors such as JQ1 and OTX015. It showed similar results.
Hetero-bifunctional compound with a BRD4 binding group and a ubiquitin E3 ligase binding group, resulting in BRD4 ubiquitylation and degradation.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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