Shelf life (days): 1460.0
Formulation: A solid
Formal Name: rel-2-[[6-[[5-chloro-2-[(3R,5S)-3,5-dimethyl-1-piperidinyl]-4-pyrimidinyl]amino]-1,2-dihydro-1-methyl-2-oxo-3-quinolinyl]oxy]-N-methyl-acetamide
Purity: ≥95%
Formula Markup: C24H29ClN6O3
Formula Weight: 485.0
CAS Number: 2166387-65-9
Notes: BI-3802 is a degrader of Bcl-6 with a half-maximal degradation concentration (DC50) value of 20 nM in SU-DHL-4 B cell lymphoma cells.{66886} It binds to Bcl-6 in a cell-free assay and inhibits the interaction of Bcl-6 with nuclear receptor co-repressor 1 (NCOR1) in a reporter assay (IC50s = ≤3 and 43 nM, respectively). BI-3802 induces Bcl-6 polymerization, as well as SIAH1-dependent ubiquitination of Bcl-6, in cell-free assays.{66887} It induces expression of the Bcl-6 target genes PTPN6 and RAPGEF1 in SU-DHL-4 cells in a concentration- and time-dependent manner.{66886} BI-3802 enhances decreases in tumor volume and weight induced by the c-Abl, Bcr-Abl, PDGFR, and c-Kit inhibitor imatinib (Item No. 13139) in a GIST-T1 gastrointestinal stromal tumor mouse xenograft model.{66888}
Deutsch
English
