BI-9564

1883429-22-8

C20H23N3O3

DMSO : 7.2 mg/mL (20.37 mM; Need warming)

Epigenetics

BI-9564 is a selective, and cell-permeable BRD9 BD inhibitor, with K_d of 5.9 nM for BRD9, and IC₅₀ of > 100 uM for BET family. IC50 & Target: Kd: 20 nM (BRD9) In Vitro: BI-9564 (<5 uM) shows no activity against 324 kinases, and at 10 uM, an inhibition >40% is observed for only 2 out of 55 GPCRs. BI-9564 has antiproliferative effect on human acute myeloid eosinophilic leukemia cell line EOL-1, with EC₅₀ of 800 nM^[1]. BI-9564 shows K_d of 73 nM for BRD7, and is >10-fold more selective for BRD9 over the highly homologues bromodomain BRD7, which has been implied as a tumor suppressor and is down-regulated in cancer cells^[2]. In Vivo: BI-9564 (180 mg/kg, p.o.) shows attractive ADME/PK profiles for in vivo proof-of-concept studies. BI-9564 results in a modest but significant additional survival benefit of 2 days compared to survival of the control group in a xenograft model of human AML^[1].