Formulation: A solid
Formal Name: (2S,4R)-N-(2-(2-(4-((4-(3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)methyl)phenoxy)ethoxy)-4-(4-methylthiazol-5-yl)benzyl)-1-((S)-2-(1-fluorocyclopropane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidine-2-carboxamide
Purity: ≥95%
Formula Markup: C49H58FN9O7S
Formula Weight: 936,1
Shelf life (days): 1460
CAS Number: 2375564-55-7
Notes: ACBI1 is a proteolysis-targeting chimera (PROTAC) composed of a ligand for BRM, also known as SMARCA2, BRG1, also known as SMARCA4, and polybromo-1D (PBRM1), which are components of switch/sucrose nonfermentable (SWI/SNF) chromatin remodeling complexes, conjugated to a von Hippel-Lindau (VHL) E3 ligase ligand.{51288} It induces degradation of BRM, BRG1, and PBRM1 with 50% degradation concentration (DC50) values of 6, 11, and 32 nM, respectively, in MV4-11 acute myeloid leukemia (AML) cells. ACBI1 decreases the proliferation of MV4-11 cells (IC50 = 28 nM) but is inactive against NCI H1703 non-small cell lung cancer (NSCLC) cells, which do not express BRM or BRG1. It prevents exhaustion of isolated human CD8+ T cells when used at concentrations of 50 and 100 nM.{51289}
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