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:
Quality Level
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
Regulatory Information
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D T Saenz et al.
Leukemia, 31(9), 1951-1961 (2017-01-04)
The PROTAC (proteolysis-targeting chimera) ARV-825 recruits bromodomain and extraterminal (BET) proteins to the E3 ubiquitin ligase cereblon, leading to degradation of BET proteins, including BRD4. Although the BET-protein inhibitor (BETi) OTX015 caused accumulation of BRD4, treatment with equimolar concentrations of
Maria Pia Abruzzese et al.
Journal of hematology & oncology, 9(1), 134-134 (2016-12-03)
Anti-cancer immune responses may contribute to the control of tumors after conventional chemotherapy, and different observations have indicated that chemotherapeutic agents can induce immune responses resulting in cancer cell death and immune-stimulatory side effects. Increasing experimental and clinical evidence highlight
Global Trade Item Number
| SKU | GTIN |
|---|---|
| SML3423-25MG | 04065268781111 |
| SML3423-5MG | 04065268781128 |