BI-9564

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BI-9564 (BI9564) 是一种有效、选择性、细胞渗透性且无细胞毒性的 BRD9 bromodomain 抑制剂，IC50 为 75 nM，Kd <20 nM。

BI-9564? (BI9564) is a potent, selective, cell-permeable and noncytotoxic BRD9 bromodomain inhibitor with IC50 of 75 nM, Kd of <20 nM; displays 45-fold selectiveity over BRD7, and >5,000-fold over BRD4-BD1, BRD4-BD2, and BRD2-BD1; blocks EOL-1 cell proliferation with EC50 of 0.8 uM, and displays antitumor activity in an AML xenograft model.

BI-9564 (<5 μM) shows no activity against 324 kinases, and at 10 μM, 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. BI-9564 shows Kd 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.

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.

BI 9564 | BI9564

Chromatin/Epigenetic

Bromodomain

BRD7|BRD9|CECR2

Cancer

——

1883429-22-8

353.4149

C20H23N3O3

>98% (HPLC)

DMSO: 7.2 mg/mL (Need warming)

O=C1N(C)C=C(C2=CC(OC)=C(CN(C)C)C=C2OC)C3=CC=NC=C13

4-(4-((dimethylamino)methyl)-2,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one

(-20℃)

With Ice Pack

≥ 2 years