SML2934

VZ185

≥98% (HPLC)

• Synonym(e): (2S,4R)-N-(2-(5-(4-(2,6-Dimethoxy-4-(2-methyl-1-oxo-1,2-dihydro-2,7-naphthyridin-4-yl)benzyl)piperazin-1-yl)pentyloxy)-4-(4-methylthiazol-5-yl)benzyl)-1-((S)-2-(1-fluorocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidine-2-carboxamide, VZ 185, VZ-185
• Empirische Formel (Hill-System): C₅₃H₆₇FN₈O₈S
• CAS-Nummer: 2306193-61-1
• Molekulargewicht: 995.21
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: −20°C
• SMILES string: FC8(CC8)C(=O)N[C@@H](C(C)(C)C)C(=O)N1[C@@H](C[C@H](C1)O)C(=O)NCc2c(cc(cc2)c7[s]cnc7C)OCCCCCN3CCN(CC3)Cc4c(cc(cc4OC)c5c6c([c]([n](c5)C)=O)cncc6)OC
• InChI: 1S/C53H67FN8O8S/c1-33-46(71-32-57-33)34-11-12-35(27-56-48(64)42-26-37(63)29-62(42)50(66)47(52(2,3)4)58-51(67)53(54)14-15-53)43(23-34)70-22-10-8-9-17-60-18-20-61(21-19-60)31-41-44(68-6)24-36(25-45(41)69-7)40-30-59(5)49(65)39-28-55-16-13-38(39)40/h11-13,16,
• InChI key: ZAGCLFXBHOXXEN-JPTLTNPLSA-N

Beschreibung

Biochem/physiol Actions

Potent and selective PROTAC degrader that targets BRD7/9 for von Hippel-Lindau (VHL) ubiquitin ligase complex-mediated degradation.

VZ185 is a potent and selective bromodomain proteins BRD7 and BRD9 degrader that targets BRD7/9 for von Hippel-Lindau (VHL) ubiquitin ligase complex-mediated degradation. VZ185 effectively induces cellular BRD7/9 degradation (by 90% BRD7 & 86% BRD9 in 4 h in HeLa cells, by 84% BRD7 in 2 h in RI-1 cells; BRD7/9 IC50 = 4.5/1.76 nM in 8 h in RI-1 cells) and exerts potent cytotoxicity in BRD9-dependent cancer cultures (IC50 = 3.389 nM/EOL-1 & 39.81 nM/A-204 post 7-day treatment).

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable