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
• Empirical Formula (Hill Notation): C₄₆H₄₇ClN₈O₉S
• CAS Number: 1818885-28-7
• Molecular Weight: 923.43
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD29472237
• Assay: ≥98% (HPLC)
• Form: powder

Properties

• Quality Segment: 100
• 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

Description

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.

Safety Information

• Storage Class: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable