BI-3802

• CAT Number: I019940
• CAS Number: 2166387-65-9
• Molecular Formula: C₂₄H₂₉ClN₆O₃
• Molecular Weight: 484.98
• Purity: ≥95%
• Storage: Store at -20°C
• IUPAC Name: 2-[6-[[5-chloro-2-[(3R,5S)-3,5-dimethylpiperidin-1-yl]pyrimidin-4-yl]amino]-1-methyl-2-oxoquinolin-3-yl]oxy-N-methylacetamide
• InChI: 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+
• InChIKey: GXTJETQFYHZHNB-GASCZTMLSA-N
• SMILES: CC1CC(CN(C1)C2=NC=C(C(=N2)NC3=CC4=C(C=C3)N(C(=O)C(=C4)OCC(=O)NC)C)Cl)C

BI-3802 (Cat No.: I019940) is a highly efficient degradation product of oncogenic transcription factor BCL6, which has a strong inhibitory effect on target genes and antiproliferative effects. BI-3802 can inhibit the BTB domain of BCL6 with an IC50 value ≤3nM. BI-3802 has antitumor activity.

Reference

[1]. Kerres N, et al. Chemically Induced Degradation of the Oncogenic Transcription Factor BCL6. Cell Rep. 2017 Sep 19;20(12):2860-2875.[2]. Mikołaj Słabicki, et al. Small-molecule-induced polymerization triggers degradation of BCL6. Nature. 2020 Nov 18.