BI-3802

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. 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. It induces expression of the Bcl-6 target genes PTPN6 and RAPGEF1 in SU-DHL-4 cells in a concentration- and time-dependent manner. BI-3802 enhances decreases in tumor volume and weight induced by the c-Abl, Bcr-Abl, PDGFR, and c-Kit inhibitor imatinib (Cay-13139) in a GIST-T1 gastrointestinal stromal tumor mouse xenograft model.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. CAS Number: 2166387-65-9. Molecular Formula: C24H29ClN6O3. Formula Weight: 485.0. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Slightly soluble: 0.1-1 mg/ml, DMSO: Sparingly soluble: 1-10 mg/ml. SMILES: CN1C2=CC=C(NC3=NC(N4C[C@H](C[C@H](C4)C)C)=NC=C3Cl)C=C2C=C(C1=O)OCC(NC)=O. InChi Code: InChI=1S/C24H29ClN6O3/c1-14-7-15(2)12-31(11-14)24-27-10-18(25)22(29-24)28-17-5-6-19-16(8-17)9-20(23(33)30(19)4)34-13-21(32)26-3/h5-6,8-10,14-15H,7,11-13H2,1-4H3,(H,26,32)(H,27,28,29)/t14-,15+. InChi Key: GXTJETQFYHZHNB-GASCZTMLSA-N.